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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 | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $1,670 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $2,180 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $2,800 | 8-10 weeks | 8-10 weeks |
| 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 | p38α (dog):5.0 nM (ki), p38β:3.6 nM (ki), JNK1:11480 nM (ki), JNK2:39 nM (ki), p38δ:2600 nM (ki), p38α:0.5 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 |
| Smiles | O=C1N(C)C(NCC(N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4.Cl.Cl |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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