Organometallic Ligands

<p>GC 376 is an inhibitor of the main protease Mpro (3CLpro) in coronaviruses as well as picornaviruses. This broad-spectrum antiviral compound has been used as investigational veterinary drug for treatment of feline infectious peritonitis virus (FIPV) infections. Recent studies also showed that GC 376 inhibits the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.03 μM and EC50 of 3.37 μM.</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>Hydroxyl radical scavenger; anti-vasospastic</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>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>Inhibitor of caspases; broad spectrum</p>

<p>A small molecule inhibitor with high selectivity for CDK8 over CDK19. Increases IL-10 production in stimulated human and murine macrophages and dendritic cells. Modulatory action on inflammatory responses has therapeutic potential.</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>Meloxicam is a non-steroidal anti-inflammatory drug (NSAID) which is used to treat various types of pain and inflammation caused by arthritis. It is also a COX-2 inhibitor which reduces gastrointestinal effects of this drug. Inhibiting these enzymes, allow for a decrease in inflammatory symptoms.</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>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>A serotonin reuptake inhibitor with anticholinergic activity and mild inhibitory activity on noradrenaline reuptake. Paroxetine has been used for the treatment of depression, anxiety disorders, post-traumatic stress disorder, premenstrual dysphoric disorder and obsessive-compulsive disorder.  Also inhibits nitric oxide synthase and cytochrome isoenzyme P450 2D6.</p>

<p>Partial agonist of D2 and D3 dopamine receptors; anti-psychotic</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>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>γ-secretase inhibitor; inhibits notch signaling</p>

<p>Antagonist of α-adrenoceptors; vasoactive agent</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>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>DNA alkylating agent; highly potent metabolite of nemorubicin</p>

<p>Potent agonist of a1β1γ1 5′-adenosine monophosphate-activated protein kinase (AMPK). It binds to the allosteric drug and metabolite (ADaM) site at the α- and β- subunit interface of AMPK. It has potential for the treatment of diabetic nephropathy. PF 06409577 reduces infections caused by flaviviruses, mediated by changes in the metabolism of lipids in host cells.</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>Inhibits JAK1 and JAK2 kinases</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>Receptor tyrosine kinase inhibitor; anti-angiogenesis; anti-oncogenesis</p>

<p>L-type calcium channel blocker</p>

<p>Ondansetron is a serotonin 5-HT3 receptor antagonist that is used to prevent vomiting and nausea in patients undergoing chemotherapy. This drug blocks the initiation of the vomiting reflex.</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>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>Sphingosine-1-phosphate (S1P) receptor agonist; antineoplastic, immunosppressant</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>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>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>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>Beta-adrenoceptor antagonist; anti-hypertensive</p>

<p>Bremelanotide is a 7 amino acid peptide that is used to treat hypoactive sexual desire disorder in premenopausal women. This drug is an agonist of many melanocortin receptors. Although, its mechanism is unknown, it is said to increase melanin expression which aids in the regulation of sexual arousal.</p>

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

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

<p>Antagonist of platelet activating factor</p>

<p>Inhibitor of Rho-kinases</p>

<p>Tandospirone is a psychotropic drug that acts as a selective serotonin receptor partial agonist. It is derived from a synthetic source, specifically targeting the 5-HT1A receptors in the brain. Tandospirone modulates serotonergic neurotransmission by binding to these receptors, which are associated with mood regulation. This action results in the anxiolytic and antidepressant effects observed with the drug.</p>

<p>RIPK2 protein kinase inhibitor; EGFR inhibitor</p>

<p>Lumiracoxib is a COX-2 selective non-steroidal anti-inflammatory drug that is used for the treatment of osteoarthritis. This drug inhibits prostaglandin synthesis via inhibition of COX-2.</p>

<p>A reversible inhibitor of IGF-1R kinase and insulin receptor. Has anti-growth effects in mesenchymal, epithelial and hematopoietic tumor types. Synergistic with other cytotoxic, hormonal and targeted anti-cancer therapy.</p>

<p>Indomethacin is a nonsteroidal anti-inflammatory drug that inhibits the production of prostaglandin PGE2. It is used to treat pain, fever, and inflammation. Indomethacin's mechanism of action is not well understood, but it may be due to interference with the ability of PMNs to bind to the surface of bacteria or to release reactive oxygen species. The drug has been shown to reduce mitochondrial membrane potential in mammalian cells, leading to apoptosis. This effect on mitochondria may also contribute to Indomethacin's anti-inflammatory effects. Indomethacin 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>Carvediol is a nonselective beta-adrenoceptor blocking agent and an alpha 1-adrenoceptor blocker. It can be used as a drug, belonging to the class of beta blockers, in the treatment of heart failure, coronary artery disease, and hypertension. Carvedilol has been shown to reduce the risk of death in patients with heart failure and improve symptoms. Furthermore it has an effect on blood pressure by decreasing peripheral vascular resistance and mean arterial pressure. Carvedilol can be metabolized by cytochrome P450 enzymes and CYP2D6 and CYP2C9 liver enzymes.</p>

<p>Antagonist of Wnt signalling pathway by inhibiting the activity of Porcn, a member of the membrane-bound O-acyltransferase (MBOAT) family. Porcn is required for the palmitoylation of Wnt, mediating its secretion and signalling. Inhibits self-renewal in embryonic stem cells, whilst promoting differentiation to epiblast stem cells.</p>

<p>Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.</p>

<p>Bestatin is a competitive protease inhibitor. It inhibits aminopeptidase N and is being studied for the use and treatment for acute myelocytic leukemia.</p>

<p>LOXO-305 is a small molecule inhibitor, which is a synthesized chemical compound designed to selectively target specific enzymes or pathways. Its source is rooted in medicinal chemistry and pharmacological research aimed at elucidating pathways involved in oncogenesis.</p>

<p>Bruton's tyrosine kinase antagonist; reduces Fcγ receptor signaling</p>

<p>Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.</p>

<p>Selective c-Met kinase inhibitor</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>Agonist of calcium sensing receptor CASR; calcimimetic agent</p>

<p>Prostaglandin D2 receptor antagonist</p>

<p>Interleukin-13 human is a recombinant cytokine, which is derived from the expression of the human IL-13 gene in suitable host systems, such as E. coli or mammalian cells. This cytokine belongs to the interleukin family and plays a pivotal role in the immune response by modulating inflammatory pathways. The mode of action of interleukin-13 involves binding to specific cell surface receptors, IL-13Rα1 and IL-13Rα2, which facilitates the activation of various intracellular signaling cascades, including the JAK/STAT pathway. This promotes the differentiation and proliferation of certain immune cells, influencing the production of IgE and contributing to the regulation of inflammatory responses.</p>

<p>ÎŽ opioid receptor agonist; anti-nociceptive; anti-depressant</p>

<p>Anastrozole is a non-steroidal drug that belongs to the class of aromatase inhibitors. It inhibits the production of estrogen by blocking the conversion of androgens to estrogens in peripheral tissues. The drug has been shown to be effective in treating breast cancer in postmenopausal women. In vitro assays have shown that Anastrozole can inhibit tumor growth as well as induce apoptosis in human serum cells, which suggests that it may be effective against a variety of cancers.</p>

<p>Thioglycosyl Naphthalimide is a highly potent human O-GlcNAcase (hOGA) inhibitor with good selectivity against human β-N-acetylhexosaminidase B (HsHexB).</p>

<p>Fingolimod is a sphingosine 1-phosphate receptor modulator that is used in the treatment of relapsing-remitting form of multiple sclerosis. It is also being studies to manage lung complications in patients with COVID-19. This drug binds to various sphingosine 1-phospahte receptors and suppresses the exit of lymphocytes from lymph nodes.</p>

<p>Androgen receptor antagonist</p>

<p>Antagonist of nociceptin receptors</p>

<p>Inhibitor of ERK1 and ERK2 kinases</p>

<p>5-HT1A serotonin receptor agonist; alleviates symptoms of depression</p>

<p>Inhibits type III tyrosine kinases (PDGFRα, PDGFRβ, FLT3)</p>

<p>CXCR3 antagonist</p>

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

<p>Acecelofenac is a non-steroidal anti-inflammatory drug that is used in the treatment of osteoarthritis, arthritis, and ankylosing spondylitis. This drug is also a cyclooxygenase inhibitor and works by inhibiting this enzyme so that pain and inflammation is reduced.</p>

<p>γ-secretase inhibitor; reduces amyloid-β in brainÂ</p>

<p>Cis/trans-form of GK 563 [2351820-19-2]</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>Pantoprazole is a proton pump inhibitor drug that is used to treat erosive esophagitis and promotes healing of tissue damage caused by gastric acid. It is used for the management of GERD. Through the proton pump inhibition, the formation of hydrochloric acid is inhibited thus inhibiting gastric secretion.</p>

<p>Histamine (H2) receptor antagonist</p>

<p>Pasireotide acetate is a synthetic cyclic peptide and a somatostatin analogue, which is derived from the chemical synthesis based on the structure of native somatostatins. It operates by binding to somatostatin receptors with high affinity, primarily targeting the sst1, sst2, sst3, and sst5 receptor subtypes. This binding inhibits the secretion of adrenocorticotropic hormone (ACTH), which can modulate the excess production of cortisol in conditions such as Cushing’s disease.</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>A potent inhibitor of STING protein (stimulator of interferon genes), a protein that partakes in intracellular DNA sensing pathway.  H 151 blocks palmitoylation of STING, which is required for the formation of multimeric complexes for recruiting downstream signalling molecules. Inhibition of STING by H 151 reduces pro-inflammatory cytokine synthesis.</p>

<p>Histamine (H2) receptor antagonist; treats ulcers and acid reflux</p>

<p>Sphingosine-1-phosphate receptor modulator</p>

<p>KBU2046 is an antimicrobial peptide, which is derived from natural or synthetic peptide sequences with potential therapeutic properties. It exerts its effects by disrupting the structure and integrity of bacterial cell membranes through the formation of pores or micelles. This action alters membrane permeability, ultimately leading to cell lysis and death.</p>

<p>17:0-20:4 Pi (4,5) P2 is a synthetic phosphoinositide, which is a chemically defined lipid derived from laboratory synthesis. It features a specific acyl chain composition with a heptadecanoic acid (17:0) at the sn-1 position and an arachidonic acid (20:4) at the sn-2 position. This phosphoinositide mimics naturally occurring phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), an essential component of cellular membranes.</p>

<p>Inhibits MET, VEGFR1-3, Tie and Ron tyrosine kinases; antineoplastic</p>

<p>Dopamine D2 receptor antagonist</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>