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ADAMTS-5 inhibitor 8

Names

[ CAS No. ]:
1394122-20-3

[ Name ]:
ADAMTS-5 inhibitor 8

[Synonym ]:
N-({(2R)-1-[4-(3-Buten-1-ylamino)-6-({[2-(2-thienyl)-1,3-thiazol-4-yl]methyl}amino)-1,3,5-triazin-2-yl]-2-pyrrolidinyl}methyl)-4-propylbenzenesulfonamide
Benzenesulfonamide, N-[[(2R)-1-[4-(3-buten-1-ylamino)-6-[[[2-(2-thienyl)-4-thiazolyl]methyl]amino]-1,3,5-triazin-2-yl]-2-pyrrolidinyl]methyl]-4-propyl-

Biological Activity

[Description]:

ADAMTS-5 inhibitor 8 is a highly potent and selective inhibitor of metalloprotease ADAMTS-5 with IC50 of 30 nM, >50-fold selectivity against ADAMTS-4 and >1000-fold selectivity against ADAMTS-1/13, MMP-13 and TACE; inhibits aggrecanase-mediated (374)ARGS neoepitope release from aggrecan and glycosaminoglycan in response to IL-1β/OSM stimulation.

[References]

References 1. Deng H, et al. J Med Chem. 2012 Aug 23;55(16):7061-79. View Related Products by Target Matrix Metalloproteinase (MMP)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
821.9±75.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H36N8O2S3

[ Molecular Weight ]:
624.844

[ Flash Point ]:
450.8±37.1 °C

[ Exact Mass ]:
624.212341

[ LogP ]:
4.46

[ Vapour Pressure ]:
0.0±3.0 mmHg at 25°C

[ Index of Refraction ]:
1.641

Related Compounds