| Omarigliptin (MK-3102) Chemical Properties |
| Boiling point | 529.4±60.0 °C(Predicted) |
| density | 1.61±0.1 g/cm3(Predicted) |
| storage temp. | 2-8°C(protect from light) |
| solubility | insoluble in EtOH; insoluble in H2O; ≥17.15 mg/mL in DMSO |
| form | solid |
| pka | 9.11±0.60(Predicted) |
| color | White to off-white |
| InChI | InChI=1S/C17H20F2N4O3S/c1-27(24,25)23-7-10-6-22(8-16(10)21-23)12-5-15(20)17(26-9-12)13-4-11(18)2-3-14(13)19/h2-4,7,12,15,17H,5-6,8-9,20H2,1H3/t12-,15+,17-/m1/s1 |
| InChIKey | MKMPWKUAHLTIBJ-ISTRZQFTSA-N |
| SMILES | [C@H] 1(C2=CC(F)=CC=C2F)OC [C@H] (N2CC3=CN(S(C)(=O)=O)N=C3C2)C [C@@H] 1N |
| CAS DataBase Reference | 1226781-44-7 |
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 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).