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TG6-10-1

更新时间:2024-01-10 17:40:07

常用名 TG6-10-1 CAS号 1415716-58-3
价格 ¥需询单/1kg ¥需询单/1g ¥需询单/1mg 纯度 98.0%
备货期 需询单 库存 询单
 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℃

供应商信息

上海楼岚生物科技有限公司

认证状态:未认证供应商
电话:52996696
地址:沪南路2729弄1310号
地区: 上海市 上海市 浦东新区
联系人:孙先生
联系人电话:021-52996696
邮件:sales@lollanechem.com
网址:http://www.bioll.com
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参考价格:$158/10mM*1mLinDMSO
其他供应商价格:
2025-02-05 TG6-10-1
价格:¥7000.9
2024-07-15 (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:需询单
2021-04-03 TG6-10-1
价格:¥2646.0

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