AMG-548

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

AMG-548 是一种有效的选择性 p38α 抑制剂，Ki 为 0.5 nM，对 p38β 表现出弱抑制作用 (Ki=3.6 nM)，选择性比 p38γ 和 p38δ 高 5,000 倍以上；与其他 36 种激酶相比，选择性高出 1,000 倍以上，并且对急性和慢性关节炎模型有效。类风湿性关节炎停产

AMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ; shows >1,000-fold selectivity over other 36 kinases, and is efficacious in acute and chronic models of arthritis. Rheumatoid Arthritis Discontinued.

AMG-548 shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=61 nM). AMG-548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC50=3 nM) and IL1b (IC50=7 nM) as well as TNFa induced IL-8 (IC50=0.7 nM) and IL-1b induced IL-6 (IC5050=1.3 nM) in human whole blood. AMG-548 (10 μM) inhibits the hDvl2 shift.

AMG-548 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.

AMG548

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

Inflammation/Immunology

Rheumatoid Arthritis

864249-60-5

461.569

C29H27N5O

>98% (HPLC)

——

Cn1c(=O)c(c(nc1NC[C@H](Cc2ccccc2)N)c3ccncc3)c4ccc5ccccc5c4

2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone

(-20℃)

With Ice Pack

≥ 2 years