AMG-548 dihydrochloride_product_DataBase

Bioactivity	AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].
Invitro	AMG-548 dihydrochloride 对 p38γ (Ki=2600 nM) 和 p38δ (ki=4100 nM) 表现出 >1000 倍的选择性。AMG-548 dihydrochloride 对 JNK2 (ki=39 nM) 和 JNK3 (ki=61 nM) 具有适度的选择性。AMG-548 dihydrochloride 在抑制全血 LPS 刺激的 TNFa (IC50=3
In Vivo	AMG-548 dihydrochloride 在大鼠生物利用度 F 为 62％，狗 F 为 47％。在大鼠中的半衰期 t1/2 为 4.6 小时，在狗中为 7.3 小时[1]。
Name	AMG-548 dihydrochloride
Formula	C29H29Cl2N5O
Molar Mass	534.48
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alphaprotein. Curr Med Chem. 2005;12(25):2979-94. [2]. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94.

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