MK-1421

Names

[ Name ]:
MK-1421

[Synonym ]:
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

Biological Activity

[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.

[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

Chemical & Physical Properties

[ 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

Related Compounds

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