Organometallic Ligands

<p>Inhibitor of leucine-rich repeat kinase LRRK2Â</p>

<p>Inhibitor of isocitrate dehydrogenase 2</p>

<p>Azumolene is a muscle relaxant drug, which is a synthetic derivative of dantrolene originating from hydantoin. The mode of action of Azumolene involves the inhibition of calcium ion release from the sarcoplasmic reticulum of skeletal muscle fibers. By impeding this release, Azumolene effectively reduces muscle contraction, thereby acting as a potent muscle relaxant.</p>

<p>Mianserin is a tetracyclic antidepressant drug that has antihistaminic and hypnosedative properties. It is used to treat depression in adults and children, as well as other disorders such as chronic pain and irritable bowel syndrome. This drug’s mechanism of action is not fully understood but is said to block alpha-adrenergic, histamine H1 and serotonin receptors.</p>

<p>Methotrexate is a chemotherapeutic and immunosuppressive medication, which is a synthetic analog of folic acid. Its source is through chemical synthesis, mimicking the structure of dihydrofolate in order to exert its effects. Methotrexate acts primarily by inhibiting the enzyme dihydrofolate reductase (DHFR), leading to a decrease in tetrahydrofolate production. This disruption in folate metabolism results in the inhibition of DNA, RNA, and protein synthesis, which affects rapidly dividing cells.Methotrexate is employed broadly in clinical oncology as an antineoplastic agent, particularly in the treatment of leukemias, lymphomas, breast cancer, and osteosarcoma. Additionally, it serves as a cornerstone for managing autoimmune diseases such as rheumatoid arthritis and psoriasis, where it helps modulate the aberrant immune response. The dual role of Methotrexate in oncology and immunosuppression underscores its versatility and critical importance in therapeutic regimens. However, its use demands careful monitoring due to potential adverse effects on non-cancerous cells and organ systems, necessitating precise dosage management and patient evaluation.</p>

<p>Inhibits actin polymerization</p>

<p>Specific inhibitor of the ubiquitin specific protease-7 (USP7), which is a validated deubiquitinase of the E3 ubiquitin-protein ligase MDM2. The compound inhibits the USP7 deubiquitinase activity by binding to acidic amino acid residues important for the interaction with ubiquitin. Induces tumor cell death and enhances cytotoxicity of chemotherapeutic agents.</p>

<p>Vanilloid receptor 1 antagonist</p>

<p>Inhibitor of p38 kinase</p>

<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>Short acting monoamine oxidase inhibitor</p>

<p>AZD9567 is a selective glucocorticoid receptor modulator (SGRM), which is a synthetic pharmaceutical compound. Its source is rooted in medicinal chemistry efforts to design ligands that selectively interact with glucocorticoid receptors. The mode of action of AZD9567 involves binding to glucocorticoid receptors with high specificity, modulating their activity to trigger anti-inflammatory and immunomodulatory responses while minimizing common side effects associated with traditional glucocorticoids.</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>Opioid receptor antagonist</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>(2R)-Arimoclomol maleate is an investigational pharmaceutical compound, which is an orally bioavailable small molecule with pharmacological activity primarily targeting cellular protein homeostasis mechanisms. This therapeutic agent is derived from molecular chaperones and operates by selectively enhancing the expression of heat shock proteins (HSPs). The mechanism of action involves the modulation of the heat shock response, wherein (2R)-Arimoclomol maleate amplifies the natural cellular defense pathways against protein misfolding and aggregation.</p>

<p>Angiotensin II receptor antagonist</p>

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