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产品描述： 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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靶点：
Ki: 0.013 μM (human recombinant DP2); 0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2);GPR; ProstaglandinReceptor |
体内研究：
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) |
参考文献：
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 |
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溶解性：
Soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.871 ml |
14.353 ml |
28.705 ml |
| 5 mM |
0.574 ml |
2.871 ml |
5.741 ml |
| 10 mM |
0.287 ml |
1.435 ml |
2.871 ml |
| 50 mM |
0.057 ml |
0.287 ml |
0.574 ml |
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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。 |
上海工商
北京