1. Metabolic Enzyme/Protease
  2. CETP
  3. MK-8262

MK-8262 

Cat. No.: HY-132303
Handling Instructions

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.

For research use only. We do not sell to patients.

MK-8262 Chemical Structure

MK-8262 Chemical Structure

CAS No. : 1432054-03-9

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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].

IC50 & 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].

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

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].

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

Molecular Weight

724.57

Formula

C₃₅H₂₅F₉N₂O₅

CAS No.
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Storage

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

References
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MK-8262
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HY-132303
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