MK-8262 T38908
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
25 mg | 1432054-03-9 | ¥10,600.00 | 询底价 |
Product Introduction
Bioactivity
英文名: MK-8262
描述: MK-8262, an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor (IC 50 = 53 nM, log D = 5.3), is a bistrifluoromethyl analogue that shows promise in research related to high-density lipoprotein (HDL) and low-density lipoprotein (LDL) with potential implications for coronary heart disease (CHD).
体外活性: MK-8262 (Compound 87) reduces cell viability in a dose-dependent manner beginning at ~10 μM in all 8 cell lines regardless of human CYP expression or glutathione depletion (HEK293/CYP cell lines expressing human CYP1A2, CYP2E1, CYP2D6, CYP2C8, CYP2B6, CYP3A4, CYP2C19, or CYP2C9)[1]. MK-8262 has no effect on human CYP protein concentration or Nrf2 activation in any of the 8 cell lines[1].
体内活性: MK-8262 (Compound 87; 10 mg/kg; orally) results in a significant HDL cholesterol increase in a 2-week chronic treatment of CETP transgenic mice[1]. MK-8262 (1 mg/kg; iv) has a T 1/2 MRT of 6 hours, a CL of 2.6 mL/min?kg, and a V ss of 0.95 L/kg for mouse[1]. MK-8262 (2 mg/kg; po) has a C max of 0.43 μM and an AUC of 7.9 μM?h for mouse[1]. MK-8262 (1 mg/kg; iv) has a T 1/2 MRT of 13 hours, a CL of 3.1 mL/min?kg, and a V ss of 2.4 L/kg for mouse[1]. MK-8262 (2 mg/kg; po) has a C max of 0.4 μM and an AUC of 9.7 μM?h for mouse[1].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: MK8262 | MK-8262 | MK 8262
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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