MK-8262 

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^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

724.57

C₃₅H₂₅F₉N₂O₅

1432054-03-9

O=C(O)C1=CC=C(C2=CC(C3=CC=C(C(F)(F)F)C=C3[C@@H]4CC[C@]5([H])N4C(O[C@@H]5C6=CC(C(F)(F)F)=CC(C(F)(F)F)=C6)=O)=C(OC)N=C2)C(C)=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Petr Vachal, et al. Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties. J Med Chem. 2021 Aug 10.  [Content Brief]