| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S86686-1mg |
≥98% | ￥360.00 |
货期：3-5天 | - | - | - | - |
|
S86686-5mg |
≥98% | ￥910.00 |
货期：3-5天 | - | - | - | - |
|
S86686-10mg |
≥98% | ￥1600.00 |
货期：3-5天 | - | - | - | - |
|
S86686-50mg |
≥98% | ￥4400.00 |
货期：3-5天 | - | - | - | - |
|
S86686-100mg |
≥98% | ￥7030.00 |
货期：3-5天 | - | - | - | - |
|
| 产品描述： | GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities | ||||||||||||||||||||
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| 靶点： | 5-HT1A Receptor:9.4 (pKi);5-HT1B Receptor:8.5 (pKi);5-HT1D Receptor:9.7 (pKi);D2 Receptor:6.3 (pKi);D3 Receptor:6.7 (pKi);5-HT2A Receptor:6 (pKi);5-HT2B Receptor:6.3 (pKi);5-HT2C Receptor:5.8 (pKi);Human 5-HT6 Receptor:<5.3 (pKi);Human 5-HT7 Receptor:6.8 (pKi);DopamineReceptor;5-HTReceptor | ||||||||||||||||||||
| 体外研究： | GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9). At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8) | ||||||||||||||||||||
| 体内研究： | In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg | ||||||||||||||||||||
| 参考文献： | 1. Leslie CP, et al. Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist. J Med Chem. 2010 Dec 9;53(23):8228-8240. | ||||||||||||||||||||
| 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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