948842-66-8

948842-66-8 structure

Name: BMS-751324
Chemical Name: Bms-751324
CAS Number: 948842-66-8
Molecular Formula: C₃₂H₃₅N₆O₁₀P
Molecular Weight: 694.628
Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
Create Date: 2020-01-20 13:40:56
Modify Date: 2024-01-12 08:11:10
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.

Name	Bms-751324
Synonyms	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

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