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Synonym: (2′S,3′S,3aR,5′R,6aS,9R,9aS,10aR)-1,3a,4,4′,5′,6a,7,8,9,9a,10,10a-Dodecahydro-9-hydroxy-3′,9,10a-trimethyl-5′-spiro[dicyclopenta[a,d]cyclooctene-3(2H),2′(3′H)-furan]-6-carboxaldehyde CAS Number: 4611-05-6 Empirical Formula (Hill...
An analog of PGJ2, potentially biologically active, and stabilized in vivo.
An acetylated form of L-carnitine that facilitates the uptake of acetyl CoA into mitochondria during fatty acid oxidation, enhances acetylcholine production, and stimulates protein and membrane phospholipid synthesis.
A constituent of the Chinese herb Artemisia identified as having anticoagulant, hypolipidemic, vasorelaxant, antioxidant, and anti-inflammatory actions in experimental models.
A long-acting sulfonylurea that inhibits KATP channels in pancreatic β-cells (IC50 = 3 nM), which leads to the release of insulin; increases the activity of intracellular insulin receptors and prevents insulin receptor downregulation during chronic insulin stimulation through a...
Selective inhibitor of CYP2C9 (Ki = 0.3 μM); inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis.
A glycopeptide antibiotic identified for its utility in the treatment of gram-positive bacteria, including penicillin-resistant staphylococci; binds to bacterial cell wall precursors, interfering with their synthesis.
Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for...
Molecular Formula: C13H15IN2O2
A mixture of the natural macrocyclic lactones avermectin B1a and avermectin B1b that has both insecticidal and anthelmintic actions.
This is a Type II pyrethrin and a potent inhibitor of calcineurin (protein phosphatase 2B). More recent study disputes its effectiveness as a calcineurin inhibitor. May also have varied effects on ion channels. Deltamethrin is a type II semi-synthetic pyrethrin, which acts as a potent inhibitor of...
A long-chain saturated fatty acid that does not affect plasma total cholesterol or LDL-cholesterol but may reduce HDL-cholesterol.
A potent HDAC8 inhibitor (IC50 = 0.01 μM) with >200-fold selectivity over HDAC isoforms 1, 2, 3, 6, and 10 (IC50s = 4, >50, >50, 2.9, and 13 μM, respectively); induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias (GI50s = 2.4 - 4 μM).
An inhibitor of the cyclin-dependent kinases Cdk1/cyclin B, Cdk2/cyclin E, and Cdk4/cyclin D1 (Kis = 1-3 nM); inhibits tumor cell proliferation (IC50s ≤ 0.6 µM in vitro), inducing cell cycle arrest and apoptosis as well as reducing phosphorylation of the retinoblastoma protein.
Anastrozole is a third generation aromatase inhibitor that suppresses synthesis of estrogen. Anastrozole exhibits anticancer chemotherapeutic activity and is clinically used to treat ER-positive breast cancer. In vitro, anastrozole inhibits proliferation of cancer cells by disrupting the...
A urinary metabolite of (±)14(15)-EET which is elevated in pregnancy-induced hypertension.
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