1432054-03-9

1432054-03-9 structure

Name: MK-8262
Chemical Name: MK-8262
CAS Number: 1432054-03-9
Molecular Formula: C₃₅H₂₅F₉N₂O₅
Molecular Weight: 724.57
Catalog: Signaling Pathways Metabolic Enzyme/Protease CETP
Create Date: 2021-10-13 09:37:04
Modify Date: 2024-01-09 16:04:28
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].

Name	MK-8262

Description	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].
Related Catalog	Research Areas >> Cardiovascular Disease Research Areas >> Metabolic Disease Signaling Pathways >> Metabolic Enzyme/Protease >> CETP
Target	IC50: 53 nM (CETP)[1]
In Vitro	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].
In Vivo	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 T1/2 MRT of 6 hours, a CL of 2.6 mL/min•kg, and a Vss of 0.95 L/kg for mouse[1]. MK-8262 (2 mg/kg; po) has a Cmax of 0.43 μM and an AUC of 7.9 μM•h for mouse[1]. 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[1]. MK-8262 (2 mg/kg; po) has a Cmax of 0.4 μM and an AUC of 9.7 μM•h for mouse[1].
References	[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.

Molecular Formula	C₃₅H₂₅F₉N₂O₅
Molecular Weight	724.57

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