Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 stimulated TNFα (IC50: 3 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | Inquiry | $ 166.00 | |
5 mg | Inquiry | $ 495.00 | |
10 mg | Inquiry | $ 821.00 | |
50 mg | Inquiry | Inquiry | |
100 mg | Inquiry | Inquiry |
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 stimulated TNFα (IC50: 3 nM). |
Targets&IC50 | JNK2:39 nM (ki), JNK1:11480 nM (ki), p38β:3.6 nM (ki), p38α (dog):5.0 nM (ki), p38α:0.5 nM (ki), p38δ:2600 nM (ki), p38γ:4100 nM (ki), JNK3:61 nM (ki) |
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]. |
Synonyms | AMG-548 dihydrochloride |
Molecular Weight | 534.48 |
Formula | C29H29Cl2N5O |
CAS No. | T10298L2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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