1226781-44-7
1226781-44-7 structure
- Name: Omarigliptin
- Chemical Name: Omarigliptin
- CAS Number: 1226781-44-7
- Molecular Formula: C17H20F2N4O3S
- Molecular Weight: 398.427
- Catalog: Biochemical Inhibitor Proteases DPP-4 inhibitor
- Create Date: 2018-04-04 08:00:00
- Modify Date: 2025-08-22 11:05:58
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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).
| Name | Omarigliptin |
|---|---|
| Synonyms |
UNII-CVP59Q4JE1
(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 MK-3102 Omarigliptin (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 2H-Pyran-3-amine, 2-(2,5-difluorophenyl)-5-[2,6-dihydro-2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-, (2R,3S,5R)- 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). |
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| Related Catalog | |
| References |
| 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 |
| Storage condition | -20℃ |
| Precursor 5 | |
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| DownStream 0 | |