Torcetrapib,262352-17-0

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YZ剂描述：

产品名称：Torcetrapib

产品别名：托彻普

英文别名：CP-529414

靶点：CETP

CAS：262352-17-0

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Torcetrapib是一种CETPYZ剂，IC50为37 nM，提高血浆中HDL-C，降低nonHDL-C。用Torcetrapib处理H295R细胞24小时或48小时都能看到Torcetrapib可以剂量依赖的增加醛固酮的释放，其EC50大约为80 nM。这种效应能被钙离子通道调节，就像钙通道阻滞剂能完全阻断torcetrapib诱导的肾上腺皮质类脂醇的释放和钙的增加。在H295R 细胞系中，Torcetrapib (1 μM)能显著增加生成类固醇基因，CYP11B2和CYP11B1的表达。

溶解性：DMSO ：30 mg/mL (50 mM)

体外研究：

Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment with an EC50 of approximately 80 nM, this effect is mediated by calcium channel as calcium channel blockers completely blocks torcetrapib-induced corticoid release and calcium increase. Torcetrapib (1 μM) significantly increases the expression of steroidogenic gene, CYP11B2 and CYP11B1, in H295R cell lines.

体内研究：Torcetrapib ( Torcetrapib results in an increase of 72.1% in high-density lipoprotein cholesterol and a decrease of 24.9% in low-density lipoprotein cholesterol, in addition to an increase of 5.4 mm Hg in systolic blood pressure, a decrease in serum potassium, and increases in serum sodium, bicarbonate, and aldosterone, in patients at high cardiovascular risk after 12 months' treatment. Torcetrapib increases HDL cholesterol levels by 50% and 60% at dose of 60 mg daily and 120 mg daily, respectively, in both healthy and moderately hyperlipidemic subjects. Torcetrapib 60 mg daily increases HDL-mediated net cholesterol efflux from foam cells primarily by increasing HDL concentrations, whereas 120 mg daily torcetrapib increases cholesterol efflux both by increasing HDL concentration and by causing increased efflux at matched HDL concentrations. Torcetrapib (90 mg/kg/day) results in a 70% inhibition of CE transfer in rabbits fed an atherogenic diet. Torcetrapib (90 mg/kg/day) increases mean HDL-C levels by above 3-fold and apoA-I levels by 2.5-fold in plasma in rabbits fed an atherogenic diet. Torcetrapib-treated animal has a multiple-fold increase in HDL-C AUC and a corresponding reduction in aortic lesion area with 60% reduction of aortic free cholesterol (FC) and cholesteryl ester (EC) in rabbits fed an atherogenic diet. Torcetrapib-treated rabbits stimulate free cholesterol efflux to a significantly greater extent than does sera from control rabbits.

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