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AMG-548
Catalog No. T10298LCas No. 864249-60-5
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].
AMG-548
Catalog No. T10298LCas No. 864249-60-5
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 | Price | Availability | Quantity |
|---|---|---|---|
| 10 mg | $126 | 35 days | |
| 25 mg | $297 | 35 days | |
| 100 mg | $1,150 | 35 days |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Targets&IC50 | p38α:0.5 nM （ki）, p38δ:2600 nM （ki）, p38γ:4100 nM （ki）, JNK1:11480 nM （ki）, JNK2:39 nM （ki）, p38α (dog):5.0 nM （ki）, p38β:3.6 nM （ki）, JNK3:61 nM （ki）, CK1: |
| 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 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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