Organometallic Ligands

<p>Fluvastatin is a statin that lowers blood cholesterol and triglycerides by inhibiting HMG-CoA reductase, an enzyme that plays a critical role in the synthesis of cholesterol. Fluvastatin has also been shown to reduce the incidence of myocardial infarction, and to reduce atherosclerotic lesions in animal models, reducing the incidence of cardiovascular disease. Fluvastatin also has been shown to inhibit the activation of toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS), which may be related to its anti-inflammatory effects. Furthermore, through lowering blood cholesterol, Fluvastatin also inhibits tubulointerstitial injury and prevents renal damage caused by high concentrations of the lipid.</p>

<p>Apixaban is an anticoagulant agent used for the prophylaxis of stroke and deep vein thrombosis leading to pulmonary embolism. This drug is an inhibitor of factor Xa and prothrominase. As a result, this prevents the formation of a thrombus.</p>

<p>Rosuvastatin is a drug that belongs to the group of statins. It is used for the treatment of high cholesterol and as an adjunct therapy for patients with coronary heart disease. Rosuvastatin reduces serum cholesterol by inhibiting HMG-CoA reductase, which is the rate-limiting enzyme in the production of cholesterol. Furthermore, this drug has been shown to have anti-inflammatory properties, which may be due to its ability to inhibit prostaglandin synthesis.</p>

<p>Required for blood coagulation</p>

<p>Kifunensine is a small molecule inhibitor that was designed and synthesized to inhibit plant and animal α-mannosidase I. It is a potent and specific inhibitor with IC50 in nanomolar range. It inhibits the enzyme isoforms in Golgi apparatus (GMI) and endoplasmatic reticulum (ERMI). The compound prevents mannose trimming on glycoproteins and shifts the glycoform content from complex to oligomannose type. Used for the production of recombinant therapeutic glycoproteins with mannose rich N-linked glycans.</p>

<p>Histone acetyltransferase inhibitor of p300/CBP; anti-proliferative</p>

<p>Hydroxyl radical scavenger; anti-vasospastic</p>

<p>Etoposide is a cytotoxic drug used in cancer chemotherapy. It inhibits DNA replication through inhibition of DNA topoisomerase II, thus catalysing cell cycle arrest and apoptosis. <br>Etoposide is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>As a synthetic trifluorinated glucocorticoid receptor agonist, Fluticasone exhibits anti-inflammatory properties. When binding to and activating glucocorticoid receptors, Fluticasone initiates the activation of lipocortin which inhibits cytosolic phospholipase A2. Consequently, the cascade of inflammatory mediator synthesis reactions are inactivated and the production of inflammatory cells namely mast cells, dendritic cells, macrophages and eosinophils and the cytokines that they produce are greatly reduced.It is this anti-inflammatory role which has enabled Fluticasone to successfully treat conditions such as asthma, emphysema, allergic rhinitis and atopic dermatitis. It has also been seen to increase anti-inflammatory effects of annexoin-1 and mitogen-activated kinase phosphatase-1; reduce mucus gland secretions and increase the number of beta-2 receptors on smooth muscles of the airways.<br>Fluticasone is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Mitomycin C is a cytotoxic agent that belongs to the class of mitomycins. It has been used for the treatment of a range of cancers and for ocular surface diseases, such as the glaucoma surgery trabeculectomy. In this case it is administered to reduce post-operative scarring which could otherwise lead to failure of the procedure. Mitomycin C is an alkylating antibiotic that inhibits DNA synthesis by cross-linking the DNA double helix. Mitomycin C also stimulates the production of transforming growth factor β1 (TGF-β1) and basic fibroblast growth factor (bFGF). Clinically, mitomycin can be used both intravenously and topically, and has been studied in a range of wound healing models.</p>

<p>7-Prenyloxycoumarin is a naturally occurring compound, often categorized as a phytochemical, which is primarily isolated from various plant sources including the Rutaceae family. This compound exhibits intriguing biochemical properties due to its unique molecular structure, primarily the presence of a prenyloxy group attached to the coumarin core. The mode of action of 7-Prenyloxycoumarin primarily involves its ability to interact with biological membranes and proteins, leading to modulation of enzymatic activity and disruption of pathogen cell walls.</p>

<p>Selective TRPM8 channel blocker. Inhibits icillin-induced store-operated Ca2+ entry, hence TRPM8 activation, in pulmonary vasculature. Reduces frequency of volume-induced contraction of bladder. Reduces micturition and nociceptive reflex actions in the bladder, suggesting therapeutic potential for bladder hypersensitivity disorders.</p>

<p>SR 4835 is a synthetic compound, which is an advanced molecular entity derived from extensive medicinal chemistry efforts. This compound exhibits a novel mechanism of action, targeting specific cellular pathways implicated in disease processes. SR 4835 functions by modulating enzyme activity, thus influencing intracellular signaling cascades that play a critical role in pathophysiological conditions.</p>

<p>(5Z)-7-Oxozeaenol is a potent and selective small-molecule inhibitor, primarily characterized as a natural product derived from fungal sources. It specifically targets and inhibits transforming growth factor-beta (TGF-β) type I receptor kinase, also known as activin receptor-like kinase 5 (ALK5), as well as TAO kinases. The inhibition occurs through covalent modification, which results in the suppression of downstream signaling pathways that are crucial in various cellular processes.</p>

<p>Autophagy inhibitor that selectively targets the StART domain of GRAMD1A</p>

<p>Pan-EGFR inhibitor (HER1, HER2 and HER4); antineoplastic</p>

<p>Ponalrestat is an aldose reductase inhibitor, which is a synthetic compound developed for pharmacological purposes. It originates from chemical synthesis designed to target and inhibit the enzyme aldose reductase effectively. The mode of action involves the competitive inhibition of aldose reductase, an enzyme involved in the polyol pathway of glucose metabolism. By preventing the reduction of glucose to sorbitol, it reduces sorbitol accumulation associated with diabetic complications.</p>

<p>Pitolisant is an inverse agonist and antagonist of the histamine (H3) receptor. It acts as an allosteric modulator of the H3 receptor to increase the activity of histamine at the M1 receptor. Pitolisant has been used in the treatment of narcolepsy, schizophrenia and Alzheimer's disease. Its mechanism of action involves binding to the amide group on histamine, which increases its affinity for the H3 receptor and enhances its activity at this site. Pitolisant has been shown to improve cognitive ability and reduce fatigue in patients with Alzheimer's disease.</p>

<p>NMDA receptor antagonist</p>

<p>Androgen receptor antagonist; therapy for endometriosis</p>

<p>Inhibitor of folate synthesis; folic acid analogue</p>

<p>Inhibitor of c-Met kinase</p>

<p>Selective partial GABAA receptor antagonist of subtypes  α1, α2, α3, α5 subunits. Non-sedative anxiolytic effects demonstrated in vivo, without compromising motor activity. Anti-nociceptive and anti-inflammatory activities also demonstrated in vivo.</p>

<p>Nilotinib is a kinase inhibitor that is used for the treatment of Chronic Myeloid Leukemia (CML). This drug is also used for the treatment of CML that is resistant to imatinib. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It also inhibits PDGFR and c-kit.</p>

<p>Anti-diabetic and anti-obesity drug.  We also have the heavy labelled material, CRB1301886.<br>Cymit Quimica provides this product solely for uses within the scope of any statute or law providing for an immunity, exemption, or exception to patent infringement (“Exempted Uses”), including but not limited to 35 U.S.C. § 271(e)(1) in the United States, the Bolar type exemption in Europe, and any corresponding exception to patent infringement in any other country. It is the sole responsibility of the purchaser or user of this product, and the purchaser or user of this product agrees to engage only in such Exempted Uses, and to comply with all applicable intellectual property laws and/or regulations. The purchaser of this product agrees to indemnify Cymit Quimica against all claims in connection with the performance of the respective commercial agreement (e.g. supply agreement) and possible infringements of intellectual property rights.</p>

<p>Inhibitor of PDE4 enzyme</p>

<p>Antagonist of D1-like dopamine receptor subtypes, D1 and D5 (Ki values 0.2 and 0.3 nM respectively). Agonist of serotonin receptors 5-HT1C and 5-HT2C (Ki values 6.3 nM and 9.3 nM respectively). Used to study the topography of D1 receptors in humans and animals. Reduces seizures in response to chemoconvulsants and has also been studied in other neurological disorders.</p>

<p>Levetiracetam is a modulates the activity of the synaptic vesicle protein 2A (SV2A) in the brain and is used to treat epilepsy.It is not clear exactly how Levetiracetam affects the activity of SV2A and if this is through inhibiting the release of neurotransmitters. However, it is thought to work by binding to a specific site on SV2A, which interferes with its normal function and ultimately leads to changes in exocytosis. One of the postulated mechanisms of action is that this modulates glutamate release. Levetiracetam is used to treat certain types of seizures in people with epilepsy.<br>Levetiracetam is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>(±)-Vasicine is an alkaloid compound, which is a naturally occurring, organic molecule found primarily in the plant Adhatoda vasica. This alkaloid is extracted from the leaves of the plant, which is native to parts of Asia, particularly India and Pakistan. (±)-Vasicine is known for its bronchodilatory and respiratory stimulant activities.</p>

<p>Partial agonist of D2 and D3 dopamine receptors; anti-psychotic</p>

<p>Alpha-2-adrenoceptor agonist; reduces intraocular pressure</p>

<p>Candesartan is a drug that belongs to the class of angiotensin II receptor antagonists and is used to treat hypertension. It is used in combination therapy with other drugs, such as hydrochlorothiazide and amlodipine, to lower blood pressure. Candesartan inhibits the formation of angiotensin II, the receptor which causes vasoconstriction and increased blood pressure.</p>

<p>A potent and selective c-Met inhibitor. Anti-tumour activity demonstrated in xenograft models in vivo. Forms a thioether conjugate by reacting with thiol groups in proteins. Non-small-cell lung carcinoma (NSCLC) tumour cells that overexpress c-MET have increased sensitivity to AMG458.</p>

<p>Inhibits the mitochondrial outer mebrane protein mitoNEET, anti-leukaemic</p>

<p>A selective antagonist of serotonin 5-HT2B receptors, inhibiting inositol phosphate formation and calcium release. Blocks 5-HT-induced contraction in rat stomach fundus. Reduces fecal output in vivo, upon inhibition of 5-HT2B by RS 127445, demonstrating a potential role for this receptor in colonic motility. Inhibits visceral hypersensitivity induced by restraint stress or colonic inflammation.</p>

<p>Used to treat psoriasis; teratogenic</p>

<p>γ-secretase inhibitor; inhibits notch signaling</p>

<p>Phosphodiesterase 5 inhibitor; anti-impotence drug</p>

<p>Prostaglandin E2 (EP2) receptor antagonist</p>

<p>Cisplatin, also known as cisplatinum, is a platinum-based anti-cancer agent that inhibits the EGFR, which is a receptor tyrosine kinase. It has been shown to have anti-cancer effects in melanoma cells and to inhibit tumor growth in mice. Cisplatin acts by interfering with the mechanism of DNA repairing. It loses one chloride ligand and binds to DNA to inhibit the synthesis, causing DNA damage, and thus inducing apoptosis in cancer cells. In certain studies, the use of cisplatin in combination with other metal chelators has shown improvement in the uptake of the anticancer drug. CisplatiN - Bio-X™ is part of our Bio-X™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>A brain-penetrant inhibitor of leucin-rich repeat kinase 2 (LRRK2) with IC50 = 0.76 nM and anti-parkinsonian activity. Gain-of-function mutations in LRRK2 gene lead to increased familial and idiopathic risk of developing the disease. The inhibitors of the kinase activity have therapeutic potential against Parkinson’s disease.</p>

<p>H+/K+ ATPase inhibitor</p>

<p>AR-R 17779 is a selective agonist for α7 nicotinic acetylcholine receptors (nAChRs) (Ki value = 190 nM for rat α7 receptor). This compound has use as a tool to study the function of α7 nicotinic receptors. One such study revealed a role for α7 nicotinic receptors in nicotine-mediated excitatory effects on hippocampal learning and memory. AR-R17779 reduces formation of atherosclerotic plaques and abdominal aortic aneurysms in apolipoprotein E-deficient mice.</p>

<p>Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) protein. This inhibition is on the EGFR tyrosine kinase domain, where Gefitinib bindings to the ATP-binding site. As a a tyrosine kinase inhibitor, Gefitinib blocks tumor growth and has led to its use in slowing the progression of non-small cell lung cancer. Gefitinib also inhibits invasion and metastasis through inhibition of macrophage receptor interacting protein kinase 2 (RIPK2), rather than EGFR.</p>

<p>DNA alkylating agent; highly potent metabolite of nemorubicin</p>

<p>A chemical probe for the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1). GNE 371 binds TAF1 with an IC50 of 10 nM and is selective over other bromodomain family members. Exerts anti-proliferative effects in synergy with BET inhibitor JQ1.</p>

<p>Phosphodiesterase inhibitor</p>

<p>PYR-41 is a small molecule inhibitor, which is sourced from chemical synthesis. It functions primarily by targeting ubiquitin-activating enzymes, particularly the E1 enzyme, to disrupt the ubiquitination process. This mechanism effectively hampers the transfer of ubiquitin to substrate proteins, thereby modulating protein degradation and signaling pathways.</p>

<p>CXCR2 antagonist</p>

<p>alpha-adrenoceptor agonist; nasal decongestant</p>

<p>BX471 hydrochloride is a selective antagonist of the C-C chemokine receptor type 1 (CCR1), which is synthesized through rigorous chemical processes. It operates by inhibiting the binding of chemokines to the CCR1 receptor, thus interfering with the signaling pathways that lead to inflammation and immune responses. This mechanism is specifically effective in modulating immune system functions and controlling pathophysiological responses in various tissue types.</p>

<p>Proteosome inhibitor; pro-apoptotic; has anti-myeloma activity</p>

<p>Inhibits JAK1 and JAK2 kinases</p>

<p>Tazarotene is an acetylenic retinoid that is used for the treatment of wrinkles, pigmentation of the skin and acne. Although, the mechanism of action for this drug is not yet fully understood, it is thought to bind to all three members of the retinoic acid receptor family. Studies have shown that this drug is associated with increased collagen production.</p>

<p>Amlodipine is a calcium channel blocker that is used to treat hypertension and angina. This drug inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle.</p>

<p>Roflumilast is a selective phosphodiesterase-4 inhibitor that is used for the treatment of exacerbations in patients with chronic obstructive pulmonary disease (COPD). It is also used to treat plaque psoriasis. This drug has anti-inflammatory and immunomodulatory effects as it aids in increasing levels of cAMP.</p>

<p>Potent inverse agonist of peroxisome proliferator-activated receptor PPARβ and PPARδ with IC50 value of 27 nM. In mouse myoblasts, DG 172 enhanced recruitment of transcriptional corepressor and down-regulated transcription of PPARβ/δ target gene Angptl4. DG 172 also possess a PPARβ/δ-independent activity on bone marrow cells and promotes dendritic cell differentiation.</p>

<p>AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with binding affinity of 1.6 nM, 6-fold selective for MTC1 over MCT2.</p>

<p>Receptor tyrosine kinase inhibitor; anti-angiogenesis; anti-oncogenesis</p>

<p>Calcitriol is a steroid hormone, vitamin D metabolite and agonist of vitamin D receptor (VDR), also known as calcitriol receptor. It regulates absorption of calcium from intestine, resorption of bone calcium and calcium excretion via kidneys. This compound also controls cell cycle, promotes cell differentiation, triggers apoptosis and acts as anti-inflammatory factor within the tumor microenvironment. It has anti-proliferative effects in malignant epithelial cells and in tumour-derived endothelial cells (TDEC). Also, it is a potent inhibitor of retinal neoangiogenesis in vitro.</p>

<p>Cis/trans-form of GK 563 [2351820-19-2]</p>

<p>Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.</p>

<p>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.</p>

<p>Irbesartan is an angiotensin II receptor antagonist that is used to treat hypertension and congestive heart failure. It is also used to delay the progression of diabetic nephropathy. This drug works to works to relax smooth muscles and lower blood pressure.</p>

<p>R-(-)-Arundic acid is a chiral compound, which is a derivative of arundic acid specifically designed for enantiomeric purity. It is sourced through synthetic organic chemistry processes, allowing for precise control over its stereochemistry. The mode of action of R-(-)-Arundic acid involves the inhibition of astrocyte activation by modulating the synthesis of certain cytokines and inflammatory mediators. This mechanism provides a neuroprotective effect, making it a valuable tool in the study of neurodegenerative diseases and brain injuries.</p>

<p>Elesclomol is an investigational anticancer agent, which is a small-molecule compound. It functions by targeting the cellular oxidative stress pathway; specifically, it enhances the production of reactive oxygen species (ROS) within cancer cells. By elevating ROS levels beyond the threshold tolerable by cancer cells, Elesclomol induces apoptosis through the disruption of mitochondrial function, making it selective for environments with heightened oxidative stress.</p>

<p>Tetrabenazine is a drug that has been used for the treatment of Parkinson's disease. It acts by inhibiting dopamine release and reducing the activity of nerve cells in the brain. Tetrabenazine Bio-X is used to treat dyskinesias, that are abnormal and involuntary muscle movements by inhibiting the monoamine transporter (VMAT2).<br>Tetrabenazine is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use."</p>

<p>Inhibits DNA topoisomerase II; antineoplastic; immunomodulatory; antimicrobial</p>

<p>Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.<br>Sorafenib is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Prasugrel is a thienopyridine prodrug that inhibits the enzyme ADP-dependent P2Y purinergic receptor. Prasugrel inhibits platelet aggregation and the formation of blood clots by blocking the conversion of ADP to ATP on the surface of platelets, thus preventing the release of serotonin from platelets. The reaction products formed by prasugrel are similar to those formed by clopidogrel and include hydrogen sulfate ions and a thiol-containing metabolite. It has also been shown to have potent cytotoxic activity against melanoma cells and anti-inflammatory properties. <br>Prasugrel is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Pitolisant is an inverse agonist and antagonist of the histamine (H3) receptor. It acts as an allosteric modulator of the H3 receptor to increase the activity of histamine at the M1 receptor. Pitolisant has been used in the treatment of narcolepsy, schizophrenia and Alzheimer's disease. Its mechanism of action involves binding to the amide group on histamine, which increases its affinity for the H3 receptor and enhances its activity at this site. Pitolisant has been shown to improve cognitive ability and reduce fatigue in patients with Alzheimer's disease.<br>Pitolisant is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&amp;D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.</p>

<p>Inhibitor of clathrin-mediated endocytosis (CME) and ligand to the clathrin heavy chain (CHC). ES9-17 is an inhibitor of the CHC function with EC50 of 13 μM in plant model Arabidopsis thaliana. ES9-17 is a non-protonophoric CME inhibitor and it does not alter the cytoplasmic pH levels substantially. In a mammalian cell line HeLa, ES9-17 reduced the uptake of transferrin, which is a CME-driven process.</p>

<p>Padsevonil is an investigational antiseizure medication, which is a synthetic pharmaceutical compound. It is derived from extensive medicinal chemistry research aiming to address complex seizure disorders resistant to conventional treatments. Padsevonil functions by exhibiting a dual mechanism of action. It binds to synaptic vesicle protein 2A (SV2A) with high affinity, similar to levetiracetam but with additional modulation of the benzodiazepine-sensitive gamma-aminobutyric acid-A (GABA-A) receptor. This combined activity potentiates its efficacy in stabilizing neuronal hyperactivity and dampening excitatory neurotransmission, providing a novel angle to tackle refractory seizures.</p>

<p>Selective A2 adenosine receptor agonist. Increases cardiac output in rats with acute heart failure, mediated by reduced venous resistance and raised heart rate. Demonstrates neuroprotective properties by lowering blood cell infiltrates and neuroinflammation in ischemic cerebral tissue.</p>

<p>Sparteine hydroiodide is the salt form of sparteine. This compound acts as an inhibitor of voltage-gated sodium channels. In organic chemisty, it is used for chiral synthesis.</p>

<p>Toceranib phosphate is a receptor tyrosine kinase inhibitor. Toceranib phosphate has been shown to be effective in the treatment of skin cancer and other types of cancer, including lung cancer and breast cancer. It is approved in the US as a treatment for canine mastocytoma (mast cell tumours).</p>

<p>Lacidipine is a lipophilic dihydropyridine calcium channel blocker that is used in the treatment of hypertension. This drug acts as an antihypertensive agent to dilate peripheral arteries and reduces blood pressure. Lacidipine blocks voltage-dependent L-type calcium channels.</p>

<p>Cyamemazine is a neuroleptic medication, which is a member of the phenothiazine class of compounds. It is synthesized from derivatives of phenothiazine, a group of agents primarily found in pharmaceuticals. The mode of action of cyamemazine involves antagonism at dopamine D2 receptors in the central nervous system. This inhibition of dopamine activity is the principal mechanism through which it exerts its antipsychotic effects. Due to its receptor activity, cyamemazine is used primarily in the management of various psychotic disorders, including schizophrenia and acute psychoses. It also exhibits anxiolytic properties, making it effective in treating anxiety associated with these conditions. By modulating neurotransmitter pathways, cyamemazine helps to alleviate symptoms such as hallucinations, delusions, and agitation, offering therapeutic benefit in complex neuropsychiatric cases. As an atypical antipsychotic, it provides an option for patients who may not respond adequately to other treatments. Although primarily used in a clinical setting, ongoing research continues to investigate potential wider applications and efficacy in treating other mental health issues.</p>

<p>Agonist of alpha7 subtype of nural nicotinic acetylcholine receptor</p>

<p>Partial inverse agonist of benzodiazepine sites of the GABAA receptors with anxiogenic properties. FG 7142 is a pharmacological stressor which generates anxiety in humans and in experimental animals such as rhesus monkeys and rodents. FG 7142 also reduces food intake and frequency of feeding in male and female rats.</p>

<p>Increases VEGF via heme oxygenase-1 modulation; anti-ulcer agent</p>

<p>Troxipide is a gastric cytoprotective agent that is used for the treatment of gastroesophageal reflux disease (GERD). It has anti-inflammatory, anti-ulcer and mucus secreting properties. This drug inhibits proinflammatory mediators in order to restore the normal gastric mucosa.</p>

<p>Dual COX/5-LO inhibitor; anti-inflammatory; analgesic</p>

<p>Beta-adrenoceptor antagonist; anti-hypertensive</p>

<p>HS-1371 is a selective chemical inhibitor targeting specific enzymes, which is derived from synthetic organic compounds with a high affinity for its target proteins. It functions by selectively binding to the active site of the enzyme, inhibiting its activity and subsequently influencing downstream signaling pathways within the cell. This mode of action allows researchers to dissect complex biochemical pathways and assess the impact of enzyme inhibition on cellular functions.</p>

<p>Muscarinic acetylcholine receptor agonist</p>

<p>VEGFR2 a tyrosine kinase receptor inhibitor; antineoplastic</p>

<p>Antagonist of dopamine (D2), serotonin (5-HT2A) and histamine H1 receptors</p>

<p>Inhibitor of vacuolar-type proton pump</p>

<p>Inhibitor of proteaseγ‐secretase, which allows to modulate of the activity of γ‐secretase substrates Notch, E-cadherin, ErbB4, and amyloid precursor protein (APP). The compound can inhibit the growth of tongue carcinoma cells by arresting cell cycle in G0–G1 phase, modulate the activity of Notch1 receptor and Caspase-3 protease and induce apoptosis. It was also demonstrated that this inhibitor reduces the levels of β-amyloid peptide in the brain of mice model for Alzheimer’s disease. This compound also enhances the neuronal differentiation embryonic cells.</p>