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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $166 | Backorder | |
5 mg | $495 | Backorder | |
10 mg | $821 | Backorder | |
50 mg | Inquiry | Backorder | |
100 mg | Inquiry | Backorder |
Description | AMG-548 dihydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulate |
In vitro | AMG-548 dihydrochloride has a modest selectivity against JNK2 (Ki: 39 nM) and JNK3 (Ki: 61 nM). It 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 (IC50: 1.3 nM) in human whole blood [1]. AMG-548 dihydrochloride (10 μM) inhibits the hDvl2 shift [2]. |
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 [1]. |
Alias | AMG-548 dihydrochloride |
Molecular Weight | 534.48 |
Formula | C29H29Cl2N5O |
Cas No. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
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