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-20°C, sealed storage, away from moisture
- 库存：
货期：1-2天
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MedChemExpress LLC
- CAS号：
2518299-32-4
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3170.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥900.0 |
| 规格： | 5 mg | 产品价格： | ￥2700.0 |
| 规格： | 10 mg | 产品价格： | ￥4500.0 |
| 规格： | 25 mg | 产品价格： | ￥9000.0 |
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AMG-548 dihydrochloride
CAS No. : 2518299-32-4
MCE 国际站：AMG-548 dihydrochloride
产品活性：AMG-548 dihydrochloride 是一种口服有效的，选择性 p38α 抑制剂 (Ki=0.5 nM)，对 p38β 略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有 >1000 倍的选择性。AMG-548 dihydrochloride 也有效抑制全血 LPS 刺激的 TNFα (IC50=3 nM)。AMG-548 dihydrochloride 通过直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε 来抑制 Wnt 信号传导。
研究领域：MAPK/ERK Pathway | Stem Cell/Wnt | Cell Cycle/DNA Damage
作用靶点：p38 MAPK | Casein Kinase
In Vitro: AMG-548 dihydrochloride shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 dihydrochloride has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=61 nM). AMG-548 dihydrochloride 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 dihydrochloride (10 μM) inhibits the hDvl2 shift.
In Vivo: 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.
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