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
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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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C35H25F9N2O5 |
|---|---|
| Molecular Weight | 724.57 |