AS1940477

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 p38α/p38β 抑制剂，IC50 分别为 11.2/36.5 nM，对 p38γ 和 δ 亚型没有影响 (IC50>1 uM)。

A potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM); displays no activity against a panel of 100 protein kinases, including JNK2, EGFR, Akt and Pim; inhibits LPS- or PHA-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC50=0.45 nM; PHA/TNFα, IC50=0.40 nM) in human PBMCs, also inhibits TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells; potently inhibits TNF production in whole blood (IC50=12 nM) and effectively inhibits TNFα production induced by LPS in rats with long-acting anti-inflammatory effect.

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AS 1940477 | AS-1940477

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

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928344-12-1

431.471

C24H22FN5O2

>98% (HPLC)

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O=C1C=CC(C2=C3NC[C@@H](CO)CN3N=C2C4=CC=C(F)C=C4)=NN1C5=CC=CC=C5C

6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one

(-20℃)

With Ice Pack

≥ 2 years