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.

Product information

CAS Number: 1432054-03-9

Molecular Weight: 724.57

Formula: C35H25F9N2O5

Chemical Name: 4-(5-{2-[(5S,7aS)-1-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-hexahydropyrrolo[1,2-c][1,3]oxazol-5-yl]-4-(trifluoromethyl)phenyl}-6-methoxypyridin-3-yl)-3-methylbenzoic acid

Smiles: CC1=CC(=CC=C1C1=CN=C(OC)C(=C1)C1=CC=C(C=C1[C@@H]1CC[C@H]2C(OC(=O)N12)C1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)C(F)(F)F)C(O)=O

InChiKey: VYZPBLVSILOWMJ-ASYYUYISSA-N

InChi: InChI=1S/C35H25F9N2O5/c1-16-9-17(31(47)48)3-5-23(16)19-12-26(30(50-2)45-15-19)24-6-4-20(33(36,37)38)14-25(24)27-7-8-28-29(51-32(49)46(27)28)18-10-21(34(39,40)41)13-22(11-18)35(42,43)44/h3-6,9-15,27-29H,7-8H2,1-2H3,(H,47,48)/t27-,28-,29?/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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). MK-8262 has no effect on human CYP protein concentration or Nrf2 activation in any of the 8 cell lines.

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. 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. MK-8262 (2 mg/kg; po) has a Cmax of 0.43 μM and an AUC of 7.9 μM•h for mouse. 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. MK-8262 (2 mg/kg; po) has a Cmax of 0.4 μM and an AUC of 9.7 μM•h for mouse.

Products are for research use only. Not for human use.