BI-4394

Names

[ Name ]:
BI-4394

[Synonym ]:
1H-Indole-2-carboxylic acid, 5-[3-[[[(4-carboxyphenyl)methyl]amino]carbonyl]-1-methyl-1H-pyrazol-5-yl]-, 2-ethyl ester
4-{[({5-[2-(Ethoxycarbonyl)-1H-indol-5-yl]-1-methyl-1H-pyrazol-3-yl}carbonyl)amino]methyl}benzoic acid
compound 15 [PMID: 22017539]

Biological Activity

[Description]:

BI-4394 is a highly potent, selective MMP-13 inhibitor with IC50 of 1 nM, displays >1,000 fold selectivity against nine other MMP isoforms (MMP2/14, IC50=18/8.3 uM); BI-4394 is potent in a full-length MMP-13 collagen degradation assay (IC50=11 nM) and is able to inhibit degradation of bovine nasal cartilage with an IC50 of 31 nM.

[References]

References 1. Taylor SJ, et al. J Med Chem. 2011 Dec 8;54(23):8174-87. View Related Products by Target Matrix Metalloproteinase (MMP)

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
764.4±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₂N₄O₅

[ Molecular Weight ]:
446.455

[ Flash Point ]:
416.1±32.9 °C

[ Exact Mass ]:
446.159027

[ LogP ]:
3.16

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.668

Related Compounds

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