| 货号 | 20971-5mg |
| 描述 | Pamapimod is a potent inhibitor of p38α MAP kinase (IC50 = 14 nM).1 It displays over 30-fold selectivity for p38α over p38β, has no activity against p38δ or p38γ, and has limited activity against a panel of 350 other kinases. Pamapimod blocks LPS-induced TNF-α production by monocytes and IL-1β generation in whole blood, and it inhibits spontaneous TNF-α release from synovial explants from patients with rheumatoid arthritis.2,3 It is orally bioavailable and abrogates inflammation and bone loss in an animal model of arthritis and pain in a rat model of hyperalgesia.2 Pamapimod suppresses the expression of inflammation-associated genes in primary, IL-1β-stimulated human chondrocytes.4 |
| 别名 | R 1503;Ro 4402257; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.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 kinase. J. Med. Chem. 54(7), 2255-2265 (2011). 2.Hill, R.J.,Dabbagh, K.,Phippard, D., et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: Preclinical analysis of efficacy and selectivity. J. Pharmacol. Exp. Ther. 327(3), 610-619 (2008). 3.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 species. Cell. Physiol. Biochem. 36(6), 2237-2249 (2015). 4.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 chondrocytes. Br. J. Pharmacol. 160(6), 1252-1262 (2010). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 406.4 |
| 分子式 | C19H20F2N4O4 |
| CAS号 | 449811-01-2 |
| 稳定性 | ≥ 2 years |
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