A DPP-4 inhibitor (IC50 = 1.6 nM; Ki = 0.8 nM); selective for DPP-4 over 168 proteases

MK-3102 – 25 mg

Brand:
Cayman
CAS:
1226781-44-7
Storage:
-20
UN-No:
Non-Hazardous - /

MK-3102 is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.6 nM; Ki = 0.8 nM).{37137} It is selective for DPP-4 over 168 proteases, ion channels, and enzymes with IC50 values greater than 10 µM in all assays. MK-3102 significantly reduces blood glucose levels in a dose-dependent manner in vivo in rats. It also has a long half-life (11 and 22 hours in rat and dog, respectively) making it suitable for once weekly dosing. Clinical trials demonstrate that formulations containing MK-3102 reduce plasma glucose and HbA1c in patients with type 2 diabetes mellitus (T2DM).  

 

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Description

A DPP-4 inhibitor (IC50 = 1.6 nM; Ki = 0.8 nM); selective for DPP-4 over 168 proteases, ion channels, and enzymes with IC50 values >10 µM in all assays; significantly reduces blood glucose levels in a dose-dependent manner in vivo in rats

Formal name: (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2,6-dihydro-2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine

Synonyms:  Omarigliptin

Molecular weight: 398.4

CAS: 1226781-44-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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