Omarigliptin (MK-3102)

Description:Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over allproteases tested (IC50 > 67 μM).IC50 value: 1.6 nM [1]Target: DPP-4 inhibitorin vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays. in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction).

Density:1.6±0.1 g/cm3

Boiling Point：529.4±60.0 °C at 760 mmHg

Molecular Formula：C17H20F2N4O3S

Molecular Weight：398.427

Flash Point：274.0±32.9 °C

Exact Mass：398.122406

PSA：98.83000

LogP：0.46

Vapour Pressure：0.0±1.4 mmHg at 25°C

Index of Refraction：1.689