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• 产品描述： 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

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

• 体外研究：
  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.

• 体内研究：
  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.

• 参考文献：
  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

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *