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.
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- CAS. Nr.: 1432054-03-9
- Formel: C35H25F9N2O5
- Molecular Weight:724.57
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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 (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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1432054-03-9
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Molecular Weight 724.57
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Formel C35H25F9N2O5
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SMILES
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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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