(E)-N-(2-(2-(三氟甲基)-1H-吲哚-1-基)乙基)-3-(3,4,5-三甲氧基苯基)丙烯酰胺
更新时间：2025-09-12 18:00:49
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| 常用名 | TG6-10-1 | CAS号 | 1415716-58-3 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors. IC50 value: 7.5 μMTarget: serotonin 5-HT2B receptorin vitro: TG6-10-1, an analog of TG4-155 (a prostaglandin receptor EP2 antagonist, with a relatively short plasma half-life (0.6 h) and low brain:plasma ratio (0.3) after systemic administration in mice), which has a superior pharmacokinetic profile making it suitable for more extensive testing. TG6-10-1 had negligible effect on a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s > 10 μM), except that TG6-10-1 weakly inhibited the serotonin 5-hydroxytryptamine 2B (5-HT2B) receptor with IC50 = 7.5 μM. At a high concentration (10 μM), TG6-10-1 had little or no effect on the enzymatic activity of COX-1 (7% inhibition) and COX-2 (14% inhibition), and inhibited the leukotriene B4 (LTB4) receptor BLT1 by 1% .EP2 receptor activation by PGE2 stimulates adenylate cyclase to elevate cytoplasmic cAMP level. TG6-10-1 has a competitive mechanism of antagonism of the EP2 receptor with an equilibrium dissociation constant for the antagonist-receptor complex (KB) of 17.8 nM.in vivo: TG6-10-1 displayed a plasma half-life of 1.6 h and a brain:plasma ratio of 1.6 after systemic administration (5 mg/kg, i.p.) in mice. A significant increase in survival was observed in post-SE mice that received TG6-10-1 compared with those in the vehicle group. Administration of TG6-10-1 improved 1-wk survival from 60 to 90% after SE. 物理化学性质： CAS号：1415716-58-3 常用中文名：TG6-10-1 常用英文名：TG6-10-1 分子式：C23H23F3N2O4 分子量：448.435 密度：1.2±0.1 g/cm3 沸点：631.8±55.0 °C at 760 mmHg 熔点：N/A 闪点：335.9±31.5 °C 储存条件：-20℃ |
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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：TG6-10-1
- 价格： ￥7000.9/50mg ￥1200.9/5mg ￥1600.9/10mg
- 纯度：99.0%
- 备货期：10天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：(E)-N-(2-(2-(三氟甲基)-1H-吲哚-1-基)乙基)-3-(3,4,5-三甲氧基苯基)丙烯酰胺
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
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参考价格：$158/10mM*1mLinDMSO