CP-346086 dihydrate
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| 包装规格: | 1g in glass bottle |
| 产品描述: | 基本信息 产品编号: C11658 产品名称: CP-346086 dihydrate CAS: 1262769-98-1 储存条件 粉末 -20℃ 四年 分子式: C26H26F3N5O3 溶于液体 分子量 513.51 化学名: 生物活性 产品描述 一种有效和具有口服活性的微粒体甘油三酯转移蛋白 (MTP) 抑制剂,对人和啮齿动物 MTP 的 IC50 为 2.0nM。CP-346086 dihydrate 可在体内降低血浆胆固醇和甘油三酯。 靶点 IC50: 2.0nM (MTP) 体外研究 CP-346086 (0.1-1000nM) dose-dependently inhibits human MTP-mediated triglyceride transfer between vesicles with an IC50 of 2.0nM. CP-346086 (24 h) inhibits apolipoprotein B (apoB) and triglyceride secretion (IC50=2.6nM) from Hep-G2 cells without affecting apoA-I secretion or lipid synthesis 体内研究 CP-346086 (1-100mg/kg; oral gavage once daily for 2 weeks) reduces plasma total, VLDL, and LDL cholesterol and triglycerides in mice. CP-346086 (25mg/kg; a single p.o.) results in an almost complete inhibition of Tyloxapol-induced triglyceride accumulation in fasted rats. CP-346086 (0.1-10mg/kg; a single p.o.) reduces acute plasma triglyceride in mice Animal Model: B6CBAF1J mice Dosage: 1, 2, 10, 20, 100mg/kg Administration: Oral gavage once daily for 2 weeks Result: Lowered total, VLDL, and LDL cholesterol and triglycerides dose dependently with 23%, 33%, 75%, and 62% reductions at 10mg/kg/day. |
| 保存条件: | -20℃ |
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