Ligands organométalliques

<p>Selective antagonist of the serotonin receptors 5-HT2A with subnanomolar affinity. The compound has clozapine-like anti-psychotic properties and more favourable CNS safety profile than traditional anti-psychotics. MDL 100907 has been used in studies on antisocial behaviour in mice and shown that the blockage of 5-HT2A receptors leads to decreased post-traumatic aggression and bradycardia.</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>

Inhibitor of factor Xa

<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>

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>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>Anti-microtubular agent; antineoplastic</p>