化合物RP64477 T8314

Product Introduction
Bioactivity


英文名: RP-64477

描述: RP-64477 是有效的胆固醇酯化酶酰基辅酶 A：胆固醇 O-酰基转移酶 (ACAT) 抑制剂。

体内活性: Inhibition by RP 64477 in a rabbit intestinal enzyme preparation was shown to be non-competitive with respect to the substrate oleoyl-CoA. In whole cell assays using human intestinal (CaCo-2), hepatic HepG2) and monocytic (THP-1) cell lines, RP 64477 inhibited ACAT activity with IC50s of 113, 503, and 180 nM, respectively. RP 64477 (0.03% w/w by diet) reduced significantly cholesterol absorption in cholesterol/cholic acid-fed rats from 94+/- 8% to 65 +/- 4%. In cholesterol-fed rabbits, cholesterol absorption was reduced from 72 +/- 5% to 50 +/-5% and 44 +/- 5% at dose levels of 10 and 30 mg kg-1 b.i.d., respectively. Plasma cholesterol levels were reduced dose-dependently in both cholesterol/cholic-acid-fed rats and cholesterol-fed rabbits. Neither cholesterol absorption nor plasma cholesterol levels were reduced significantly in animals maintained on standard laboratory diets. Pharmacokinetic studies indicated that RP 64477 were very poorly absorbed following oral administration to rats.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 8.33 mg/mL (16.70 mM)


关键字: Diglyceride acyltransferase | inhibit | mono- acylglycerol acyltransferase | RP-64477 | RP 64477 | Acyltransferase | Inhibitor | acyl-CoA:cholesterol acyltransferase | Diacylglycerol acyltransferase

相关产品: YM-750 | RU-SKI 43 | Xanthohumol | 24-Methylenecholesterol | 10,12-Tricosadiynoic acid | BAY-3827 | ACAT-IN-1 cis isomer | PD 128042 | BMS-986172 | Beauvericin

相关库: ReFRAME Related Library | Bioactive Compounds Library Max | Inhibitor Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library

化合物RP64477 T8314信息由TargetMol中国为您提供，如您想了解更多关于化合物RP64477 T8314报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途