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AMG-548
CAS No. 864249-60-5
AMG-548( AMG548 )
Catalog No. M16264 CAS No. 864249-60-5
AMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 119 | In Stock |
|
| 10MG | 173 | In Stock |
|
| 25MG | 409 | In Stock |
|
| 100MG | 1544 | In Stock |
|
| 200MG | 2074 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameAMG-548
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NoteResearch use only, not for human use.
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Brief DescriptionAMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ.
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DescriptionAMG-548 is a potent and selective inhibitor of p38α with Ki of 0.5 nM, dispalys weak inhibition for p38β (Ki=3.6 nM), and >5,000-fold selectivity over p38γ and p38δ; shows >1,000-fold selectivity over other 36 kinases, and is efficacious in acute and chronic models of arthritis. Rheumatoid Arthritis Discontinued.
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In VitroAMG-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). AMG-548 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 (IC5050=1.3 nM) in human whole blood. AMG-548 (10 μM) inhibits the hDvl2 shift.
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In VivoAMG-548 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.
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SynonymsAMG548
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PathwayMAPK/ERK Signaling
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Targetp38 MAPK
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Recptorp38 MAPK
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Research AreaInflammation/Immunology
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IndicationRheumatoid Arthritis
Chemical Information
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CAS Number864249-60-5
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Formula Weight461.569
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Molecular FormulaC29H27N5O
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Purity>98% (HPLC)
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Solubility——
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SMILESCn1c(=O)c(c(nc1NC[C@H](Cc2ccccc2)N)c3ccncc3)c4ccc5ccccc5c4
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Chemical Name2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Verkaar F, et al. Chem Biol. 2011 Apr 22;18(4):485-94.
2. Lee MR, et al. Curr Med Chem. 2005;12(25):2979-94.
3. Dominguez C, et al. Curr Opin Drug Discov Devel. 2005 Jul;8(4):421-30.
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