| CAS NO: | 864249-60-5 |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 生物活性 | AMG-548, an orally active and selectivep38αinhibitor (Ki=0.5 nM), shows slightly selective overp38β(Ki=36 nM) and >1000 fold selective againstp38γandp38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulatedTNFα(IC50=3 nM)[1]. AMG-548 inhibitsWntsignaling by directly inhibitingCasein kinase1isoforms δ and ε[2]. | |||||||||
| IC50& Target[1][2] |
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| 体外研究 (In Vitro) | 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[1]. | |||||||||
| 体内研究 (In Vivo) | AMG-548 has rat F of 62% and dog F of 47%. The t1/2is 4.6 hours in rats and 7.3 hours in dogs[1]. | |||||||||
| 分子量 | 461.56 | |||||||||
| 性状 | Solid | |||||||||
| Formula | C29H27N5O | |||||||||
| CAS 号 | 864249-60-5 | |||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||
| 储存方式 |
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