Organometallic Ligands

<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>Abiraterone is an anti-cancer drug that has been shown to be effective in treating prostate cancer. It works by blocking the production of testosterone by inhibiting androgen synthesis. Abiraterone does this by inhibiting CYP17A1, which converts cholesterol into pregnenolone, and then into progesterone and testosterone. Furthermore, it binds to the enzyme steroid 5-alpha reductase, which converts testosterone into dihydrotestosterone (DHT). Abiraterone is usually a last resort for patients who have stopped responding to other lines of hormone therapies, which is known as second-line therapy.</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>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>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>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>Inhibitor of IGF1 receptor</p>

<p>17-AAG is the first clinically tested hsp90 inhibitor that exhibits antitumor activity. Its antitumor effects are documented in vivo for various animal models, including erbB2-dependent breast cancer, prostate cancer models, and melanoma.</p>

<p>beta2-adrenoreceptor agonist; anti-asthmatic</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>Antagonist of cardiac potassium channel HERG; anti-psychotic</p>

<p>(R)-9BMS is a chiral boron reagent, which is synthesized through the modification of certain boronic compounds. This reagent is known for its ability to facilitate asymmetric synthesis, specifically in the enantioselective reduction of ketones. The source of (R)-9BMS involves intricate organic synthesis techniques that allow for the precise arrangement of its chemical structure, making it highly effective for its intended applications.</p>