Organometallic Ligands

<p>Agonist of motilin receptor</p>

<p>Rinvanil is a synthetic vanilloid compound, which is derived from chemical synthesis. Its primary mode of action involves the activation of the transient receptor potential vanilloid 1 (TRPV1) channels, which are found on the surface of certain sensory neurons. TRPV1 is a well-characterized receptor that plays a critical role in the sensation of pain and heat, making it a key target in the study of pain mechanisms and potential analgesics.</p>

<p>Inhibitor of panPI3K/mTOR</p>

<p>Glucocorticoid receptor agonist</p>

<p>Inhibitor of VEGFR, PDGR, c-Kit and Ret; inhibitor of angiogenesis</p>

<p>Inhibitor of factor Xa</p>

<p>5-Fluoro-1-(tetrahydro-2-furyl)uracil is a chemotherapeutic agent, which is a synthetic derivative of uracil. This compound is developed from modified nucleosides with the aim of enhancing antitumor efficacy. Its mechanism of action involves the inhibition of thymidylate synthase, leading to a disruption in DNA synthesis. By integrating into RNA and DNA, it ultimately impedes tumor cell proliferation due to RNA processing interference and DNA damage.</p>

<p>Inhibitor of glycogen synthase 3 (GSK-3) and cyclin-dependent kinases CDK1, CDK2 and CDK5. Kenpaullone can substitute transcription factor Klf4 in reprogramming of fibroblast to induced pluripotent stem cells when using the method of ectopic expression of transcriptional factors. In an in vitro model for Alzheimer’s disease, kenpaullone decreased production of amyloid beta peptides Aβ40 and Aβ42.</p>

<p>Fulvestrant is an estrogen receptor antagonist that is used in the treatment of HR+ breast cancer. This drug can be used as monotherapy or in combination with Alpelisib. Fulvestrant works both by down-regulating and by degrading the estrogen receptor.</p>

<p>Diphenidol is an antiemetic agent used for the treatment and prevention of nausea and vomiting associated with various conditions. Its mechanism of action is not well known but it is thought to diminish vestibular stimulation and depress labyrinthine function.</p>

<p>Inhibitor of EIF2AK3/PERK kinases</p>

<p>Positive allosteric modulator of the metabotropic glutamate receptor mGluR5 with EC50 in submicromolar range. The compound is able to increase mGluR5 function in vitro and in vivo. A study showed that ADX-47273 enhanced fear extinction learning as well as improved reversal learning in experimental animals.</p>

<p>Nintedanib is an anti-inflammatory and anti-cancer drug. It is used for treatment of idiopathic pulmonary fibrosis. Nintedanib is a prodrug that is rapidly converted to the active form nintedanib, which inhibits angiogenesis by interfering with the activation of vascular endothelial growth factor receptor 1 (VEGFR1). <br>Nintedanib 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 ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.</p>

<p>Arbutin or alpha-arbutin is a natural product. It is a hydroquinone glucoside with antioxidant properties. It is widely used in cosmetics as depigmenting agent, acting as an inhibitor of tyrosinase in melanocytes. Arbutin acts by supressing the enzymes that stimulate these melanocytes without killing or fully inhibiting them. As a consequence, melanin production is decreased to avoid hyperpigmentation that might be caused by an excess of UV radiation or a higher activity of tyrosinases.</p>

<p>AZD-7648 is a selective inhibitor of DNA-dependent protein kinase (DNA-PK), which is a pivotal enzyme involved in the non-homologous end joining (NHEJ) pathway of DNA repair. This product is derived from extensive chemical synthesis and optimization, designed for its specificity and efficacy in inhibiting DNA-PK activity. The mode of action involves binding to the ATP-binding site of DNA-PK, thereby obstructing its ability to facilitate the repair of double-strand DNA breaks.</p>

<p>Volasertib is an investigational small-molecule compound, which is a synthetic derivative with inhibitory activity against Polo-like kinase 1 (PLK1). PLK1 is a serine/threonine-protein kinase that plays a pivotal role in the regulation of cell cycle progression, specifically during mitosis. By inhibiting PLK1, Volasertib disrupts mitotic spindle assembly, leading to cell cycle arrest at the G2/M phase and ultimately inducing apoptosis in cancer cells.</p>

<p>Capsaicin-d3 is a deuterium-labeled analog of capsaicin, which is a stable isotope-labeled compound. It is derived from the naturally occurring alkaloid capsaicin, found in chili peppers. The deuterium labeling replaces specific hydrogen atoms with the isotope deuterium, allowing for precise tracking and quantification in various analytical applications.</p>

<p>Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin receptors. It was designed to treat mood disorders, such as depression. It has been shown to improve mood by increasing the levels of certain neurotransmitters in the brain such as dopamine and noradrenaline. Agomelatine has beneficial phase-shifting effects in humans; it causes a sleep phase advance, a drop in body temperature, and an initial release of melatonin. According to controlled human studies, Agomelatine is equally effective at treating severe depression as the SSRI antidepressants paroxetine and sertraline.</p>

<p>Full antagonist to the estrogen beta receptor (ERβ) with 36-fold selectivity for the β over α receptor. ERβ is a tumour suppressor and PHTPP is a useful tool to study the biology of estrogen-dependent tumours.</p>

<p>5-HT2A receptor antagonist</p>

<p>Inhibits non-receptor tyrosine kinase BTK; antineoplastic</p>

<p>Droperidol is a butyrophenone derivative, which is an antipsychotic agent and antiemetic medication, sourced from synthetic chemical processes. Its mode of action involves antagonism of dopamine D2 receptors in the central nervous system, particularly in the chemoreceptor trigger zone of the brain, and it also possesses some alpha-adrenergic blocking properties.</p>

<p>5-Fluorouracil is a cytotoxic drug that inhibits the synthesis of DNA. It is used in combination therapy to treat cancer and is a pyrimidine analog. This drug inhibits the formation of thymidylate synthase from uracil. As a result, this leads to DNA and RNA synthesis inhibition and cell death.</p>

<p>Nitazoxanide acts as a noncompetitive inhibitor of the pyruvate: ferredoxin/flavodoxin oxidoreductases of various microorganism with Ki values between 2 and 10 μM. Nitazoxanide is clinically relevant for its broad-spectrum action to reduce the growth of bacteria, various parasites, and especially for its efficacy against the pathogen Helicobacter pylori. Nitazoxanide also has been shown to be effective in treating inflammatory bowel disease and acute enteritis caused by bacteria. In 2021, nitazoxanide was tested for the treatment of COVID-19 patients with mild symptoms due to its broad antiviral action.</p>

<p>A novel non-covalent inhibitor of the PLpro protease from SARS-CoV-2 and SARS-CoV viruses. GRL 0617 inhibits the proteolytic processing of the viral polypeptide. As PLpro also acts as a protease in pathways involved in innate immunity, there are indications that it can promote immunity against the virus.</p>

<p>Zileuton is an inhibitor of the 5-lipoxygenase enzyme, thus preventing the leukotrienes LTE4, LDT4, LTB4 and LTC4 from being formed. This in turn reduces inflammation, bronchoconstriction and mucus secretion in the airways. As a result, Zileuton can be used in the treatment and management of asthma and allergic rhinitis. Studies have shown that Zileuton has the potential to reverse dementia-related brain damage.</p>

<p>Halogenated derivative of febrifugine; coccidiostat</p>

<p>Vasopressin analog; vasoactive agent</p>

<p>Dipeptidyl peptidase 4 (DPP4) inhibitor</p>

<p>17:0-20:4Pi (4) P is a synthetic phosphoinositide, which is a type of phospholipid. It is typically sourced from laboratory synthesis, often incorporating stable isotopes or specific fatty acid chains to mimic natural compounds found in cell membranes. This product functions primarily as a probe in biochemical experiments, particularly for studying lipid signaling pathways within cells.</p>

<p>Inhibitor of IGF1 receptor</p>

<p>Fexofenadine is a selective histamine-1 receptor antagonist that is used to treat the symptoms of seasonal allergies. It does not cross the blood-brain barrier and carries little-to-no activity at off targets. This drug binds to the inactive form of the H1 receptor and inhibits its activation and downstream effects.</p>

<p>High affinity inhibitor of glycogen synthase kinase GSK-3 with Ki of 0.6 nM. A 1070722 showed favourable characteristics for the penetration across blood brain barrier. A 1070722 was also shown to reduce the phosphorylation of microtubule-associated protein Tau.</p>

<p>Naloxone hydrochloride is a competitive antagonist at mu-, delta- and kappa-opioid receptors. Naloxone binding to receptors blocks the effects of opioids such as morphine, heroin, or oxycodone. Naloxone has been shown to be effective in treating acute overdoses of these drugs and reversing the depression of respiratory function that accompanies opioid overdose. It is also used to alleviate withdrawal symptoms and in the treatment of neonatal abstinence syndrome (NAS). NAS is a condition that occurs when infants are exposed to addictive levels of opioids in utero and go through withdrawal after birth.</p>

<p>Inhibitor of discoidin domain receptor DDR1</p>

<p>Inhibitor of BRAG2-mediated activation of Arf GTP-ase. In vitro experiments showed that Bragsin2 inhibits the Arf GTP-ase activation that is mediated by a nucleotide exchange factor BRAG2 in a membrane-dependent manner. Bragsin2 interacts with the PH domain of BRAG2 protein as well as membrane, which prevents the activation of lipidated Arf. Bragsin2 affects the trans-Golgi network and was shown to affect the tumour sphere in breast cancer cell lines.</p>

<p>SD 0006 is a small-molecule inhibitor, which is synthesized through specialized chemical processes. It functions by selectively inhibiting the cyclooxygenase-2 (COX-2) enzyme, which plays a significant role in the inflammatory pathway. This inhibition reduces the production of pro-inflammatory prostaglandins, ultimately leading to a decrease in inflammation.</p>

<p>Antagonist of cardiac potassium channel HERG; anti-psychotic</p>

<p>Medetomidine is a synthetic compound of the benzodiazepine class. It has a variety of pharmacological effects, including sedation and muscle relaxation, and is used in veterinary medicine as an anesthetic agent for animals. Medetomidine can be administered intravenously, intramuscularly, or subcutaneously. The drug crosses the blood-brain barrier to produce its sedative effect. This agent has been shown to be effective in inducing anesthesia in experimental animals with a wide range of body weights. Medetomidine has also been shown to have cardiovascular effects such as lowering systolic pressure and heart rate. Medetomidine HCl is soluble in water and trifluoroacetic acid (TFA).<br>Medetomidine HCl is rapidly hydrolyzed by esterases at physiological pH to medetomidinol (MTM) and then further metabolized by glucuronide conjugation to form medetominol glucuronide</p>

<p>Bisoprolol is a β1- adrenergic antagonist agent that is used to treat hypertension and prevent myocardial infarction. As adrenergic neurotransmitters activate β1-receptors it causes an increase in blood pressure and heart rate. By reducing contractility and the need for oxygen through competitive inhibition of β1-adrenergic receptors, bisoprolol reduces the cardiac workload.</p>

<p>Semaglutide is a peptide that is used as a pharmacological agent for the treatment of type 2 diabetes, and other diseases and is also used for long-term weight management in obesity. It is an analogue of glucagon-like peptide-1 (GLP-1) and acts as a GLP-1 receptor agonist and inhibitor of the enzyme DPP-4, which is responsible for the degradation of GLP-1. As a result, semaglutide increases levels of GLP-1, which stimulates insulin release from pancreatic beta cells. Semaglutide has been shown to reduce body weight, blood pressure and HbA1c levels in patients with type 2 diabetes, through its action to increase insulin production and inhibit the production of glucagon. Semaglutide acetate 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.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>Biperiden hydrochloride is an anticholinergic medication, which is a synthetic derivative. It exerts its effects primarily through the central nervous system by blocking acetylcholine receptors. This blockade reduces the activity of acetylcholine, a neurotransmitter, which plays a role in muscle contractions and various neural functions. By antagonizing the muscarinic receptors, Biperiden hydrochloride helps in modulating the balance between neurotransmitters in the brain.</p>

<p>Ketanserin is a 5-HT2A serotonin receptor antagonist that is used for the treatment of hypertension. This drug is also used in research to study the serotonergic system. Ketanserin has been found to also block the vesicular monoamine transporter 2.</p>

<p>Agonist of β3-adrenoreceptors with thermogenic properties and potential to control diet-induced obesity. The compound reversed obesity in adult rats and was effective even in animals that continued to feed on high-fat food. It caused the enlarged white adipocytes to shrink and triggered remodelling of the white adipose tissue.</p>

<p>3-Hydroxy-5-{[(naphthalen-2-yl)carbamoyl]amino}benzoic acid is a synthetic compound characterized by its complex molecular structure incorporating naphthalene and benzoic acid moieties. As a derivative of benzoic acid, it is typically synthesized through a series of chemical reactions designed to introduce the 3-hydroxy and carbamoyl functional groups, creating a compound with potentially unique bioactive properties.</p>

<p>PF 00835231 is an investigational viral polymerase inhibitor, which is derived from the structural optimization of existing antiviral compounds. This small molecule manifests its mechanism of action by directly inhibiting the activity of the viral RNA-dependent RNA polymerase, a crucial enzyme in the replication machinery of coronaviruses. By binding to the active site of the polymerase, PF 00835231 effectively obstructs the replication process of viral RNA, thereby limiting viral proliferation within the host.</p>

<p>mTOR serine/threonine kinase inhibitor</p>

<p>Potent and selective GSK3-β inhibitor, with IC50 value of 48 nM. Increases Nanog expression and regulates self-renewal in murine embryonic stem cells (ESCs). Induces reprograming of induced pluripotent stem cells (iPSCs) to derive cells from specific lineages.</p>

<p>Serotonin 5-HT3 receptor antagonist; anti-emetic</p>