GSK163090
更新时间：2025-08-23 14:00:06
采购访问：17次
| 常用名 | GSK163090 | CAS号 | 844903-58-8 |
|---|---|---|---|
| 价格 | 纯度 | 99.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.IC50 value: 9.4/8.5/9.7 (pKi) [1]Target: 5-HT in vitro: GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated amoderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9). [1]in vivo: Fromamong these analogues, the cyclic urea derivative, GSK163090, emerged due to its low hERG affinity and excellent in vitro DMPK profile. The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokineticprofile in rat and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL. On the basis of these results and its promising preclinical developability profile, GSK163090 was selected as an appropriate development candidate for progression toward clinical proof-of-concept studies. [1] 物理化学性质： CAS号：844903-58-8 常用中文名：GSK163090 常用英文名：GSK163090 分子式：C25H29N5O 分子量：415.531 密度：1.2±0.1 g/cm3 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃ |
上海化源世纪贸易有限公司
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商品数：396715件
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地址：上海市普陀区金沙江路1759号圣诺亚大厦B座
地区： 上海市 上海市 普陀区
联系人：徐经理
联系人电话：133 1186 9306
邮件：xuqm@chemsrc.com
网址：http://www.chemsrc.com
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- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：GSK163090
- 价格： ￥10500.9/50mg ￥1900.9/5mg ￥3300.9/10mg ￥17500.9/100mg
- 纯度：99.0%
- 备货期：10天
- 联系人：阿拉丁
2881459338
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- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：GSK163090
- 价格：
- 纯度：99.0%
- 备货期：10天
- 联系人：徐经理
351666998
复制
133 1186 9306
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参考价格：$462/10mM*1mLinDMSO