| Identification | Back Directory | [Name]
Bms751324 | [CAS]
948842-66-8 | [Synonyms]
Bms751324
BMS-751324
(BMS751324)
[[4-[5-(cyclopropylcarbamoyl)-2-methylanilino]-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carbonyl]-propylcarbamoyl]oxymethyl 2-(4-phosphonooxyphenyl)acetate
Benzeneacetic acid, 4-(phosphonooxy)-, 1-[[[[[[4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbonyl]propylamino]carbonyl]oxy]methyl] ester | [Molecular Formula]
C32H35N6O10P | [MOL File]
948842-66-8.mol | [Molecular Weight]
694.63 |
| Hazard Information | Back Directory | [Uses]
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model[1]. | [in vivo]
BMS-751324 (1 mg/kg, 3mg/kg; p.o.; twice daily for 1 week) inhibits paw swelling in rat adjuvant arthritis model, as well as (1 mg/kg, 3mg/kg; p.o.; single dose) inhibiting LPS-induced TNFα production[1].
BMS-751324 (1 mg/kg-100 mg/kg for rat, 10 or 30 mg/kg for monkey with 5 mL/kg of methocel suspension; p.o.; single dose) exhibits a bio-conversion in animals[1].
| [References]
[1] Liu C, et al. Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo [1, 2-f][1, 2, 4] triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases[J]. Journal of medicinal chemistry, 2010, 53(18): 6629-6639. |
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