产品
编 号：F745143
分子式：C35H25F9N2O5
分子量：724.57
分子式：C35H25F9N2O5
分子量：724.57
产品类型
规格
价格
是否有货
结构图
CAS No: 1432054-03-9
产品详情
生物活性：
MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log?D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.
体内研究：
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. MK-8262 (1 mg/kg; iv) has a T1/2 MRT of 6 hours, a CL of 2.6 mL/min?kg, and a Vss of 0.95 L/kg for mouse. MK-8262 (2 mg/kg; po) has a Cmax of 0.43 μM and an AUC of 7.9 μM?h for mouse. MK-8262 (1 mg/kg; iv) has a T1/2 MRT of 13 hours, a CL of 3.1 mL/min?kg, and a Vss of 2.4 L/kg for mouse. MK-8262 (2 mg/kg; po) has a Cmax of 0.4 μM and an AUC of 9.7 μM?h for mouse.
体外研究：
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). MK-8262 has no effect on human CYP protein concentration or Nrf2 activation in any of the 8 cell lines.
MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log?D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.
体内研究：
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. MK-8262 (1 mg/kg; iv) has a T1/2 MRT of 6 hours, a CL of 2.6 mL/min?kg, and a Vss of 0.95 L/kg for mouse. MK-8262 (2 mg/kg; po) has a Cmax of 0.43 μM and an AUC of 7.9 μM?h for mouse. MK-8262 (1 mg/kg; iv) has a T1/2 MRT of 13 hours, a CL of 3.1 mL/min?kg, and a Vss of 2.4 L/kg for mouse. MK-8262 (2 mg/kg; po) has a Cmax of 0.4 μM and an AUC of 9.7 μM?h for mouse.
体外研究：
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). MK-8262 has no effect on human CYP protein concentration or Nrf2 activation in any of the 8 cell lines.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备