Pamapimod
Cat. No.：YN350039
| 产品名称: | Pamapimod |
| CAS No.: | 449811-01-2 |
| Chemical Name: | 6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one |
| Synonyms: | Ro4402257; R1503 |
| 分子量: | 406.38 |
| 分子式: | C₁₉H₂₀F₂N₄O₄ |
| SMILES: | O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Pamapimod (Ro4402257) 是一种有效的，选择性和口服活性的p38 MAPK抑制剂，对于p38α和p38β的IC50分别为 14 nM 和 480 nM，Ki分别为 1.3 nM 和 120 nM。Pamapimod 对 p38δ 或 p38γ 亚型没有活性。Pamapimod 可用于类风湿关节炎和其他自身免疫性疾病的研究。 |
| IC50和靶点: | [{name:"p38α:14 nM (IC50)"},{name: "p38α:1.3 nM (Ki)"},{name: "p38β:480 (IC50)"},{name: "p38β:120 nM (Ki)"}] |
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Goldstein, D.M., Soth, M., Gabriel, T., et al.Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinaseJ. Med. Chem.54(7),2255-2265(2011)
Hill, R.J., Dabbagh, K., Phippard, D., et al.Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: Preclinical analysis of efficacy and selectivityJ. Pharmacol. Exp. Ther.327(3),610-619(2008)
Fehr, S., Unger, A., Schaeffeler, E., et al.Impact of p38 MAP kinase inhibitors on LPS-induced release of TNF-α in whole blood and primary cells from different speciesCell. Physiol. Biochem.36(6),2237-2249(2015)
Joos, H., Albrecht, W., Laufer, S., et al.Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in promary, interleukin - 1β-simulated human chondrocytesBr. J. Pharmacol.160(6),1252-1262(2010)
