AMG-548 dihydrochloride |
| Catalog No.GC38518 |
경구 활성 및 선택적 p38α 억제제(Ki=0.5nM)인 AMG-548 디히드로클로라이드는 p38β(Ki=36nM)에 대해 약간 선택적이고 p38γ 및 p38δ에 대해 >1000배 선택성을 나타낸다.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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AMG-548 dihydrochloride, a potent, 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].
AMG-548 dihydrochloride has rat F of 62% and dog F of 47%. The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1].
[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/?. Chem Biol. 2011 Apr 22;18(4):485-94.
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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