BMS-751324_product_DataBase

Bioactivity	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].
Invitro	BMS-751324 (10 μM; 0-60 min) 能够被碱性磷酸酶人胎盘 ALP 水解，而不会被酯酶水解[1]。
In Vivo	BMS-751324 (1 mg/kg, 3mg/kg; 口服; 每天 2 次, 共 1 周) 抑制大鼠佐剂性关节炎模型足肿胀，(1 mg/kg, 3mg/kg; 口服; 单剂量) 并抑制脂多糖诱导的 TNFα 的产生[1]。BMS-751324 (大鼠: 1 mg/kg-100 mg/kg, 猴子: 10 或 30 mg/kg, 5 mL/kg 甲基纤维素悬浮液; 口服; 单剂量) 在动物体内会发生生物转化，产生 BMS-582949 (HY-14305A)[1]。
Name	BMS-751324
CAS	948842-66-8
Formula	C32H35N6O10P
Molar Mass	694.63
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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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