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KR-62436

Names

[ CAS No. ]:
761414-79-3

[ Name ]:
KR-62436

[Synonym ]:
3-Pyridinecarbonitrile, 6-[[2-[[2-(5-cyano-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl]amino]ethyl]amino]-
6-[(2-{[2-(5-cyano-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl]amino}ethyl)amino]pyridine-3-carbonitrile
KR-60436 FREE BASE
6-[(2-{[2-(5-Cyano-4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl]amino}ethyl)amino]nicotinonitrile

Biological Activity

[Description]:

KR-62436 (KR62436) is a potent, selective DPP4 inhibitor with IC50 of 0.78, 0.49, 0.14 uM for rat plasma, porcine kidney, human DPP4 (Caco-2), respectively; completely inhibits DPP-IV-mediated degradation of GLP-1 in vitro at 10 uM, exhibits selectivity against several proteases including proline-specific protease; promotes primary tumor growth and lung metastasis in a 4T1 tumor allograft mouse model, also shows anti-hyperglycemic activity in vivo.

[References]

References 1. Kim KR, et al. Eur J Pharmacol. 2005 Jul 25;518(1):63-70. 2. Yang F, et al. Cancer Res. 2018 Dec 24. pii: canres.0620.2018. doi: 10.1158/0008-5472.CAN-18-0620. View Related Products by Target Dipeptidyl Peptidase (DPP)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
591.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C14H15N7O

[ Molecular Weight ]:
297.315

[ Flash Point ]:
311.6±32.9 °C

[ Exact Mass ]:
297.133820

[ LogP ]:
-1.35

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.671


Related Compounds

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