MK-3012
Omarigliptin
CAS: 1226781-44-7
Molecular Formula: C17H20F2N4O3S
MK-3012 - Names and Identifiers
MK-3012 - Physico-chemical Properties
| Molecular Formula | C17H20F2N4O3S |
| Molar Mass | 398.43 |
| Density | 1.61±0.1 g/cm3(Predicted) |
| Boling Point | 529.4±60.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 9.11±0.60(Predicted) |
| Storage Condition | 2-8°C(protect from light) |
| In vitro study | Omarigliptin is a potent DPP-4 inhibitor with high selectivity (IC50 > 67 μmol/L) and weak ion channel activity among other tested proteases, the IC50 values of Caγ1.2, and Naγ1.5 are greater than 30 μm. Omarigliptin quickly and competitively binds to the DPP-4 active site. This process is highly selective and is a reversible process. In the case of high blood sugar, omarigliptin can cause an increase in insulin levels and a decrease in glucagon levels. |
| In vivo study | In the oral glucose tolerance test (OGTT) in lean mice, oral administration of Omarigliptin 1 hour before glucose screening significantly and concentration-dependently reduced blood glucose excursions. Administration of omarigliptin concentration-dependently increases the blood concentration of the active GLP-1. Its pharmacokinetic studies in male Sprague-Dawley rats and Beagles showed that omarigliptin has a low clearance rate (0.9 − 1.1 mL/min/kg); the volume of distribution at steady state is 0.8 − 1.3 L/kg; The terminal half-life is long, about 11-22 h. In dogs and rats, the oral bioavailability of omarigliptin is high, almost 100%. During the study, omarigliptin was well tolerated and no significant changes in mortality or physiological parameters were observed. After a single oral dose of 25 mg of omarigliptin in subjects, omarigliptin was rapidly absorbed in vivo, reaching a peak concentration (Cmax) of 750 nmol/L within 1 H. In subjects, the bioavailability was ≥ 74%. |
MK-3012 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.51 ml | 12.549 ml | 25.099 ml |
| 5 mM | 0.502 ml | 2.51 ml | 5.02 ml |
| 10 mM | 0.251 ml | 1.255 ml | 2.51 ml |
| 5 mM | 0.05 ml | 0.251 ml | 0.502 ml |
Last Update：2024-01-02 23:10:35
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