Ligas Organometálicas

<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>Docetaxel is an antineoplastic agent that is used to treat various cancers such as breast and prostate cancer. This drug interferes with the normal function of microtubule growth. It is an anti-mitotic drug used in chemotherapy. Research has shown that this drug also induces programmed cell death in cancer cells.</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>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>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>(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>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>Alpha-2-adrenoceptor agonist; reduces intraocular 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>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>CXCR2 antagonist</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>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>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>Casein kinase (CK1ε and CK1Ύ) inhibitor</p>