Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and <1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
10 mg | 4-5 weeks | $ 78.00 | |
25 mg | 4-5 weeks | $ 297.00 | |
100 mg | 4-5 weeks | $ 1,230.00 |
Description | AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2]. |
Targets&IC50 | CK1:, p38β:3.6 nM (ki), JNK3:61 nM (ki), JNK1:11480 nM (ki), JNK2:39 nM (ki), p38α (dog):5.0 nM (ki), p38α:0.5 nM (ki), p38δ:2600 nM (ki), p38γ:4100 nM (ki) |
In vitro | AMG-548 (10 μM) inhibits the hDvl2 shift[2]. AMG-548 is 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]. 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). |
In vivo | The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1]. AMG-548 has rat F of 62% and dog F of 47%. |
Molecular Weight | 461.56 |
Formula | C29H27N5O |
CAS No. | 864249-60-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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AMG-548 864249-60-5 MAPK p38 MAPK AMG 548 AMG548 inhibitor inhibit