1235995-16-0
1235995-16-0 structure
- Name: MK-1421
- Chemical Name: 5-{(1R,3R)-1-(1-Ethyl-1H-pyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-β-carbolin-1-yl}-3-methyl-1,3,4-oxadiazol-2(3H)-one
- CAS Number: 1235995-16-0
- Molecular Formula: C27H24FN9O2
- Molecular Weight: 525.537
- Create Date: 2020-01-20 14:44:55
- Modify Date: 2024-04-13 16:36:53
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A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM); shows excellent efficacy in a mouse model of glucose excursion (oGTT) and demonstrates glucose-dependent release of insulin from relevant human tissue.
| Name | 5-{(1R,3R)-1-(1-Ethyl-1H-pyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-β-carbolin-1-yl}-3-methyl-1,3,4-oxadiazol-2(3H)-one |
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| Synonyms |
1,3,4-Oxadiazol-2(3H)-one, 5-[(1R,3R)-1-(1-ethyl-1H-pyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl]-3-methyl-
5-{(1R,3R)-1-(1-Ethyl-1H-pyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydro-1H-β-carbolin-1-yl}-3-methyl-1,3,4-oxadiazol-2(3H)-one |
| Description | A potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM); shows excellent efficacy in a mouse model of glucose excursion (oGTT) and demonstrates glucose-dependent release of insulin from relevant human tissue. |
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| References | References 1. Shah SK, et al. ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. View Related Products by Target Somatostatin Receptor |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 794.8±70.0 °C at 760 mmHg |
| Molecular Formula | C27H24FN9O2 |
| Molecular Weight | 525.537 |
| Flash Point | 434.5±35.7 °C |
| Exact Mass | 525.203674 |
| LogP | 0.37 |
| Vapour Pressure | 0.0±2.8 mmHg at 25°C |
| Index of Refraction | 1.791 |