| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S85425-5mg促销 |
≥98% | ￥128.00 ￥115.00 |
10 | - | - | - | - |
|
S85425-10mg促销 |
≥98% | ￥242.00 ￥217.00 |
8 | - | - | - | - |
|
S85425-25mg促销 |
≥98% | ￥558.00 ￥502.00 |
2 | - | - | - | - |
|
S85425-50mg促销 |
≥98% | ￥990.00 ￥891.00 |
4 | - | - | - | - |
|
S85425-100mg促销 |
≥98% | ￥1690.00 ￥1521.00 |
2 | - | - | - | - |
|
| 产品描述： | R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | p38α:0.2 nM (Kd);p38β:29 nM (Kd);p38MAPK;Autophagy | ||||||||||||||||||||
| 体外研究： | R1487 Hydrochloride exhibits IC50 values of 10 nM for p38α inhibition and 200 nM for the inhibition of TNFα induced production of IL-1β. R1487 (Compounds 2a) inhibits production of TNFα by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS | ||||||||||||||||||||
| 体内研究： | R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β. Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively | ||||||||||||||||||||
| 参考文献： | 1. Goldstein DM, 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].J Med Chem. 2011 Apr 14;54(7):2255-65. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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