Organometallic Ligands

<p>A potent inhibitor of phosphodiesterase type 9 (PDE9) tested in human and murine in vitro assays (IC50 values: 55 nM and 100 nM respectively). BAY 73-6691 induces long-term potentiation and improves memory in rodents. Has therapeutic potential for Alzheimer’s disease.</p>

<p>Anti-inflammatory; inducer of P450 II B family</p>

<p>Allosteric activator of AMP-activated protein kinase (AMPK) acting on the AMPK-β subunit with therapeutic potential in metabolic disorders such as diabetes, obesity, etc. A769662 also blocks the differentiation of mouse embryonic stem cells (mESCs) and maintains the mESCs in naïve state even in the absence of leukemia inhibitory factor (2i/L).</p>

<p>A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).</p>

<p>Fludarabine triphosphate trisodium is a nucleotide analog, which is a type of chemotherapy agent derived from purine nucleosides. This compound is the active metabolite of fludarabine, sourced from synthetic chemistry designed to mimic naturally occurring nucleotides involved in DNA replication. The mode of action involves its incorporation into the DNA strand during replication, where it effectively inhibits DNA polymerase and ribonucleotide reductase. This disruption impairs DNA synthesis, leading to apoptosis or programmed cell death, particularly in rapidly dividing cancer cells.</p>

<p>Inhibits tankyrase (TNKS1 and TNKS2 with IC50 values of 11 and 4 nM respectively), by binding to the catalytic poly-ADP-ribose polymerase (PARP) domain. This stabilizes cytoplasmic protein Axin, mediating β-catenin depletion and thereby suppresses Wnt signalling pathway. XAV 939 has anti-proliferative and pro-apoptotic effects on neuroblastoma and colorectal cancer cells.</p>

<p>Tacrolimus is a calcineurin inhibitor drug that is used for the prevention of rejection after an organ transplant. This drug can also be used in the treatment of severe atopic dermatitis. Tacrolimus’ mechanism of action is not well known however it is understood that this drug inhibits T-lymphocyte activation by binding to an intracellular protein called FKBP-12. This drug also has anti-inflammatory properties.</p>

<p>Loratadine is a non-sedating, inverse agonist antihistamine used for the treatment of allergic rhinitis, an IgE (immunoglobulin E) mediated disease. Loratadine binds to histamine H1 receptors, preventing histamine from binding and causing an allergic reaction.It has been found to inhibit the release of eosinophil cationic protein by acting on different components of allergic inflammation, in particular in the modulation of ICAM-1 expression on nasal epithelial cells as a mechanism of protective for the epithelium, and therefore, the damage of mucosa is reduced. In recent studies, it was found that loratadine is a potent HR1 antagonist with in vitro inhbitory effect on human mast-cell lines, HMC-1 (from mast cell leukaemia) with an IC50 between 10 and 50 μM.Loratadine 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>Malotilate is a pharmacological agent that is used to treat symptoms of hepatitis, bowel disease, and collagen diseases. This drug reduces collagen synthesis and cell migration activity of fibroblasts in vitro. It also has been shown to facilitate liver regeneration in rats.</p>

<p>Inhibitor of the Bruton tyrosine kinase</p>

<p>Ramipril is an angiotensin-converting enzyme (ACE) inhibitor. It is used in the treatment of high blood pressure, congestive heart failure and other cardiovascular diseases. Ramipril inhibits the conversion of angiotensin I to angiotensin II by blocking ACE, which lowers blood pressure and reduces fluid retention.This product 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>Opioid receptor antagonist</p>

<p>Inhibitor of PDE4 enzyme; anti-inflammatory</p>

<p>Analeptic</p>

<p>(S)-Mephenytoin is a substrate of cytochrome P450 enzyme CYP2C19 (a hydroxylase). It is an effective anticonvulsant that improves control of seizures in patients. According to studies, the drug exhibits a genetic polymorphism in CYP2C19 that results in reduced metabolism in some individuals.</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>A cytidine analogue and inhibitor of DNA methyl transferases (DNMTs) with anti-cancer activity. This stable, hydrophilic compound forms covalent complexes between DNMT and zebularine-substrate DNA. It causes DNA lesions that block replication and cause replication fork collapse, leading to the formation of DNA double-strand breaks. It was also shown that zebularine-induced DNA methylation decrease in the IL-1β promoter region and disrupts molecular mechanisms of neuroinflammation. Moreover, this molecule down-regulates the DNA-methylation profile in the pluripotency genes’ promoters, which leads to improved development of somatic cell nuclear transfer (SCNT) embryos.</p>

<p>Aminopterin is an antineoplastic agent and antifolate, which is a synthetic derivative of pteroylglutamic acid. It functions as a chemotherapeutic agent by inhibiting dihydrofolate reductase, an enzyme crucial in the folic acid pathway, thereby preventing the conversion of dihydrofolate to tetrahydrofolate. This disruption leads to impaired synthesis of purine nucleotides and thymidylate, which are essential for DNA synthesis and cell division.</p>

<p>Angiotensin II receptor antagonist</p>

<p>Dapoxetine is a serotonin reuptake inhibitor drug that is used to treat premature ejaculation. This drug works by increasing the levels of serotonin in the brain, which in turn can help to delay the reflex that triggers ejaculation. As a result, it delays ejaculation and improves control over this.</p>