產(chǎn)品目錄

規(guī)格	1mg 5mg 25mg
CAS	912806-16-7
別名
化學名	4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide hydrochloride
分子式	C22H27ClN6O2
分子量	442.94
溶解度	≥ 44.3mg/mL in DMSO with gentle warming
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

BMS-582949 hydrochloride is a novel, potent and highly selective p38α mitogen-activated protein kinase (p38α MAPK) inhibitor [1].

The p38α MAP kinase plays a critical role in regulating the production of many inflammatory cytokines, including TNF-α and IL-1β. Excessive production of TNF-α and IL-1β has been implicated in many inflammatory diseases [1].

BMS-582949 hydrochloride potently inhibited the activity of p38α MAPK with the IC50 value of 13 nM [1]. BMS-582949 showed no significant effects on cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 with the IC50 values of >40 μM. BMS-582949 weakly inhibited the activity of CYP3A4, with the IC50 value of 18-40 μM. BMS-582949 displayed >2000-fold selectivity for p38α over a diverse panel of 57 kinases, include serine kinases, receptor tyrosine kinases, nonreceptor tyrosine kinases, and the p38γ and δ isoforms. BMS-582949 showed 450-fold selectivity over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective over Raf [1]. In mice, after oral administration of BMS-582949 (10 mg/kg), the clearance rate for BMS-582949 is 4.4 mL/min/kg. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively [1].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術有限公司

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