MK-8262 is an orally active and potentcholesteryl ester transfer protein (CETP)inhibitor with anIC₅₀of 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^[1].

IC50: 53 nM (CETP)^[1]

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].

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_1/2MRT of 6 hours, a CL of 2.6 mL/minokg, and a V_ssof 0.95 L/kg for mouse^[1].
MK-8262 (2 mg/kg; po) has a C_maxof 0.43 μM and an AUC of 7.9 μMoh for mouse^[1].
MK-8262 (1 mg/kg; iv) has a T_1/2MRT of 13 hours, a CL of 3.1 mL/minokg, and a V_ssof 2.4 L/kg for mouse^[1].
MK-8262 (2 mg/kg; po) has a C_maxof 0.4 μM and an AUC of 9.7 μMoh for mouse^[1].

724.57

C₃₅H₂₅F₉N₂O₅

1432054-03-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.