| 貨號 | 規(guī)格 | 價格 | 上海 | 北京 | 武漢 | 南京 | 購買數(shù)量 |
|---|---|---|---|---|---|---|---|
S81004-5mg |
≥98% | ￥382.50 | >10 | - | - | - |
|
S81004-10mg |
≥98% | ￥660.00 | >10 | - | - | - |
|
S81004-25mg |
≥98% | ￥1309.00 | >10 | - | - | - |
|
S81004-50mg |
≥98% | ￥2050.00 | >10 | - | - | - |
|
Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as?CRTH2) antagonist. Timapiprant (OC000459) potently displaces [3H] PGD2 from human recombinant?DP2?(Ki=13 nM), rat recombinant?DP2?(Ki=3 nM), and human native?DP2?(Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils
| 產(chǎn)品描述： | Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as?CRTH2) antagonist. Timapiprant (OC000459) potently displaces [3H] PGD2 from human recombinant?DP2?(Ki=13 nM), rat recombinant?DP2?(Ki=3 nM), and human native?DP2?(Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils | ||||||||||||||||||||
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| 靶點： | Ki: 0.013 μM (human recombinant DP2); 0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2);GPR;?ProstaglandinReceptor | ||||||||||||||||||||
| 體內(nèi)研究： | Timapiprant (OC000459) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED50=0.04 mg/kg). Timapiprant (OC000459) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED50=0.01 mg/kg) | ||||||||||||||||||||
| 參考文獻： | 1. Pettipher R, Vinall SL, Xue L, Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. J Pharmacol Exp Ther. 2012 | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存條件： | -20℃ | ||||||||||||||||||||
| 配置溶液濃度參考： |
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| 注意： | 部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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營業(yè)執(zhí)照(三證合一)
北京