2. MAPK/ERK Pathway
  3. p38 MAPK
  4. BMS-582949

BMS-582949 (compound 7k) 是一种口服有效的、高度选择性的 p38α MAP 酶抑制剂，对 p38α 的IC50 为 13 nM，对 TNFα 的 IC50 为 50 nM。BMS-582949 可用于研究类风湿性关节炎。

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BMS-582949 Chemical Structure

BMS-582949 Chemical Structure

CAS No. : 623152-17-0

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BMS-582949 的其他形式现货产品:

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BMS-582949 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis[1].

IC50 & Target[1]

p38α

13 nM (IC50)

体内研究
(In Vivo)

BMS-582949 (5 mg/kg， p.o.， 90 min) 显著降低 LPS 诱导的 BALB/c 雌性急性炎症小鼠模型中 TNFα 的产生[1]。
BMS-582949 (0.3-100 mg/kg， p.o.， q.d/b.i.d) 显著减少爪肿胀[1]。
BMS-582949 静脉注射 (i.v.) 的溶解方案使用 25% 的 N-甲基吡咯烷酮，33% 的聚乙二醇 400，9% 的丙二醇和 33% 的水作为溶剂[1]。
BMS-582949 口服灌胃 (p.o.) 溶解方案使用聚乙二醇 400 作为溶剂[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: murine models of acute inflammation from BALB/c female mice[1]
Dosage: 5 mg/kg
Administration: Oral gavage (p.o.), detection content at 90 min after LPS injection
Result: Reduced the TNFα production by 89% at 2 h, by 78% at 6 h before the LPS challenge.
Animal Model: Rat adjuvant arthritis (rat AA) models from Male Lewis rats[1]
Dosage: 1, 10, 100 mg/kg, once daily (q.d)
Administration: Oral gavage (p.o.)
Result: Reduced paw swelling with dose-dependent, with efficacy observed at doses of 10 and 100 mg/kg.
Animal Model: Rat adjuvant arthritis (rat AA) models from Male Lewis rats[1]
Dosage: 0-5 mg/kg, b.i.d
Administration: Oral gavage (p.o.)
Result: Improved efficacy markedly of reduction in paw swelling at doses of 1 and 5 mg/kg.
Reduced paw swelling significantly at doses as low as 0.3 mg/kg.
Clinical Trial
分子量

406.48

Formula

C22H26N6O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BMS-582949 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

BMS-582949623152-17-0BMS582949BMS 582949p38 MAPKorally activerat adjuvant arthritis (rat AA) modelsrheumatoid arthritisInhibitorinhibitorinhibit

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