BMS-751324

Names

[ Name ]:
BMS-751324

[Synonym ]:
Benzeneacetic acid, 4-(phosphonooxy)-, α-[[[[[[4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbonyl]propylamino]carbonyl]oxy]methyl] ester
Bms-751324
({[(4-{[5-(Cyclopropylcarbamoyl)-2-methylphenyl]amino}-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl](propyl)carbamoyl}oxy)methyl [4-(phosphonooxy)phenyl]acetate

Biological Activity

[Description]:

BMS-751324 is a novel clinical prodrug of BMS-582949, which is a highly selective p38α MAPK inhibitor with IC50 of 13 nM; BMS-751324 is effectively bioconverted into parent drug BMS-582949 in vivo by alkaline phosphatase and esterase in a stepwise manner; demonstrates similar efficacy in rat LPS-induced TNFα pharmacodynamic model and rat adjuvant arthritis model compared with BMS-582949; BMS-751324 is indeed effective in addressing the pH-dependent absorption issue associated with BMS-582949.

[References]

References 1. Liu C, et al. J Med Chem. 2015 Oct 8;58(19):7775-84. View Related Products by Target p38 MAPK

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₃₂H₃₅N₆O₁₀P

[ Molecular Weight ]:
694.628

[ Exact Mass ]:
694.215210

[ LogP ]:
1.22

[ Index of Refraction ]:
1.676

Related Compounds

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