Organometallic Ligands

<p>Inhibits P-gp transporters ; modulates P-gp-mediated multidrug resistance</p>

<p>AZD9833 is an oral selective estrogen receptor degrader (SERD), which is a small molecule therapeutic synthesized by AstraZeneca. Its mode of action involves binding to the estrogen receptor, leading to the receptor's conformational change and subsequent degradation. This mechanism significantly downregulates estrogen receptor signaling, which is a crucial pathway in the progression of estrogen receptor-positive breast cancers.</p>

<p>Cis/trans-form of GK 563 [2351820-19-2]</p>

<p>L-type calcium channel blocker</p>

<p>Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.</p>

<p>Inhibitor of EGFR transmembrane receptor</p>

<p>Phosphodiesterase (PDE5, 6, 9 and 11) inhibitor</p>

<p>BI-0115 is a highly selective inhibitor for the lectin-like oxidised low-density lipoproteins (LDL) receptor 1 (LOX-1). In vitro, BI-0115 inhibits internalisation of oxidised LDL (oxLDL) with IC50 of 5.4?µM. The crystal studies revealed that BI-0115 glues two LOX-1 dimers together, resulting in blocked access of oxLDL. LOX-1 is a Ctype lectin-like receptor expressed on endothelial cells, macrophages and vascular smooth muscle. It is responsible for the regulation, internalisation and degradation of oxidised low-density lipoproteins (oxLDL). BI-0115 is a novel inhibitor to LOX-1 and is a valuable tool to study LOX-1 biology, and their role in diseases, such as, cancer and atheroschelerosis.</p>

<p>MLN 4924 is a selective small molecule that acts as an inhibitor of the Nedd8-activating enzyme. This compound is synthetically derived and functions by inhibiting the conjugation of Nedd8 to cullin proteins. By blocking this pathway, MLN 4924 disrupts the activity of the SCF (Skp, Cullin, F-box containing complex) E3 ubiquitin ligase, leading to an accumulation of proteins that can induce apoptosis and cell cycle arrest.</p>

<p>Irbesartan is an angiotensin II receptor antagonist that is used to treat hypertension and congestive heart failure. It is also used to delay the progression of diabetic nephropathy. This drug works to works to relax smooth muscles and lower blood pressure.</p>

<p>R-(-)-Arundic acid is a chiral compound, which is a derivative of arundic acid specifically designed for enantiomeric purity. It is sourced through synthetic organic chemistry processes, allowing for precise control over its stereochemistry. The mode of action of R-(-)-Arundic acid involves the inhibition of astrocyte activation by modulating the synthesis of certain cytokines and inflammatory mediators. This mechanism provides a neuroprotective effect, making it a valuable tool in the study of neurodegenerative diseases and brain injuries.</p>

<p>A prodrug of the DNA-intercalating agent daunorubicin with anti-tumoral activity, used for suicide gene therapy and activity-dependent ablation of cells. Daun02 is an inactive form of the toxin, which gets activated upon cleavage with prodrug-activating enzyme β-galactosidase, yielding daunorubicin. Genetic constructs have been designed carrying the lacZ gene, coding for β-galactosidase, under control of application-specific promoters. The cells expressing the β-gal undergo cell death since the enzyme hydrolizes the prodrug into the active toxin.</p>

<p>Selective and reversible inhibitor of the multicatalytic 26S proteasome. The inhibition of protein breakdown affects several metabolic pathways and leads to cell death. The compound is effective in treating multiple myeloma because it prevents the binding of myeloma cells to bone marrow stroma and inhibits osteoclast differentiation.</p>

<p>MK-4074 is an acetyl-CoA carboxylase (ACC) inhibitor, which is a compound originally developed by pharmaceutical research entities focusing on metabolic disorders. Acetyl-CoA carboxylase is a key enzyme in the biosynthesis of fatty acids, playing a critical role in the regulation of lipid metabolism. By inhibiting this enzyme, MK-4074 lowers the levels of malonyl-CoA, subsequently reducing fatty acid synthesis and increasing fatty acid oxidation.</p>

<p>Tetrabenazine is a drug that has been used for the treatment of Parkinson's disease. It acts by inhibiting dopamine release and reducing the activity of nerve cells in the brain. Tetrabenazine Bio-X is used to treat dyskinesias, that are abnormal and involuntary muscle movements by inhibiting the monoamine transporter (VMAT2).<br>Tetrabenazine 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>Please enquire for more information about GB1107 including the price, delivery time and more detailed product information at the technical inquiry form on this page</p>

<p>GDF-15, or Growth Differentiation Factor 15, is a cytokine, which is a type of signaling protein. It is primarily sourced from macrophages, but can also be secreted by other tissues such as the liver, heart, and adipose tissue. The protein is part of the transforming growth factor beta (TGF-β) superfamily and is involved in regulating inflammatory and apoptotic pathways.</p>

<p>Inhibits DNA topoisomerase II; antineoplastic; immunomodulatory; antimicrobial</p>

<p>Maleimide-DOTA is a chemical conjugation agent, which is a synthetic compound used in the field of radiopharmaceutical development. It is derived from the combination of maleimide and DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid). The maleimide moiety specifically reacts with thiol groups, allowing for the selective conjugation to cysteine residues of peptides or proteins. This reactivity is crucial for precise coupling in biochemical modifications, while the DOTA component serves as a versatile chelator for radiometals.</p>

<p>A potent antagonist of H2-receptor. Demonstrated effective and prolonged inhibition of gastric acid secretion after a single 100 mg or 200 mg dose in humans. Considered as a potential treatment for duodenal ulcer but incidences of idiosyncratic hepatocellular injury halted further development.</p>