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CAS No. : 1261491-89-7
MCE 国际站:Olumacostat glasaretil
产品活性:Olumacostat glasaretil (DRM01) 是乙酰辅酶 A 羧化酶 (ACC) 的小分子抑制剂。
研究领域:Metabolic Enzyme/Protease
作用靶点:Acetyl-CoA Carboxylase
In Vitro: Acetyl coenzyme A carboxylase controls the first, rate limiting step in fatty acid biosynthesis. Olumacostat glasaretil inhibits de novo lipid synthesis in primary and transformed human sebocytes. At 3 μM, olumacostat glasaretil reduces fatty acid synthesis to at or below baseline levels. 14C-acetate incorporation levels are 85%-90% lower forSEB-1 cultures treated with olumacostat glasaretil at 20 μM compared to control samples. At 3 μM, olumacostat glasaretil reduces sebocyte triacylglycerol, cholesteryl/wax ester, diacylglycerol, cholesterol and phospholipid levels from control values on average by approximately 86%, 57%, 51%, 39% and 37%, respectively.
In Vivo: Olumacostat glasaretil is a pro-drug of the ACC inhibitor 5-(tetradecyloxy)-2-furoic acid (TOFA) and is designed to enhance delivery in vivo. Topical application of olumacostat glasaretil but not TOFA significantly reduces hamster ear sebaceous gland size. HPLC analyses of hamster ear extracts shows that olumacostat glasaretil treatment increases ACC levels and the ratio of acetyl-CoA to free CoA in tested animals, indicating increased fatty acid oxidation. These changes are consistent with ACC inhibition. Matrix-assisted laser desorption/ionization (MALDI) imaging reveals that OG applied onto Yorkshire pig ears accumulates in sebaceous glands relative to the surrounding dermis. At week 12, OG treatment shows greater reductions from baseline in inflammatory lesions and noninflammatory lesions, and more patients with greater than or equal to 2-grade improvement in investigator global assessment score than vehicle.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Lipid Metabolism Compound Library | hACC2-IN-1 | Moiramide B | ND-646 | Sethoxydim | Firsocostat (S enantiomer) | CP-640186 hydrochloride | CP-610431 | ACC1/2-IN-2 | MK-4074 | Acetyl-CoA Carboxylase-IN-1 | CMS-121 | PF-05175157 | S-2E | Fluazifop-P-butyl | A-908292 | Haloxyfop | TOFA | ACC1/2-IN-1 | Propaquizafop
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货号: HY-17641
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