Omarigliptin

Product Name: Omarigliptin (MK-3102)
Synonyms: MK-3102;(2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(Methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-aMine;MK-3012;(2S,3R,5S)-2-(2,5-Difluorophenyl)-5-[2-(Methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-aMine (MK-3102 enantioMer);(2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine;OMarigliptin;OMarigliptin (MK-3102);2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine MK3102
CAS: 1226781-44-7
MF: C17H20F2N4O3S
MW: 398.43
EINECS: 682-558-0
Boiling point: 529.4±60.0 °C

Omarigliptin/MK-3102 is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.6 nM; Ki = 0.8 nM). It is selective for DPP-4 over 168 proteas es, 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).
Omarigliptin is a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor to be used as treatment for type 2 diabetes

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