貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S87213-5mg	99.0%	￥590.00 S87213-5mg ￥590.00 現(xiàn)貨	6 6	-	-	-
S87213-10mg	99.0%	￥990.00 S87213-10mg ￥990.00 現(xiàn)貨	6 6	-	-	-
S87213-25mg	99.0%	￥1590.00 S87213-25mg ￥1590.00 現(xiàn)貨	6 6	-	-	-
S87213-50mg	≥98%	￥2530.00 S87213-50mg ￥2530.00 2-3天	0 貨期：2-3天	-	-	-
S87213-100mg	≥98%	￥3970.00 S87213-100mg ￥3970.00 2-3天	0 貨期：2-3天	-	-	-

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產(chǎn)品介紹

BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease

產(chǎn)品描述：

靶點(diǎn)：

p38α MAPK:13 nM (IC50);TNFα:50 nM (IC50, in cells);p38MAPK;Autophagy

體外研究：

BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM.
BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms.

體內(nèi)研究：

BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency. Animal Model: Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model. Dosage: 1, 10, 100 mg/kg. Administration: Orally once daily (from day 11 to day 19). Result: Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.

參考文獻(xiàn)：

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 Med Chem. 2010 Sep 23;53(18):6629-39.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.258 ml	11.288 ml	22.576 ml
5 mM	0.452 ml	2.258 ml	4.515 ml
10 mM	0.226 ml	1.129 ml	2.258 ml
50 mM	0.045 ml	0.226 ml	0.452 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。

參考文獻(xiàn)

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BMS-582949 (hydrochloride)

BMS-582949; BMS 582949; BMS582949; PS-540446; PS 540446; PS540446.