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TG6-10-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TG6-10-1图片
CAS NO:1415716-58-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
TG6-10-1 是一种 EP2 拮抗剂,仅针对 EP2 显示出低纳摩尔的拮抗剂活性,比人 EP3、EP4 和 IP 受体高 300 倍以上的选择性,比 EP1 受体高 100 倍的选择性。
Cas No.1415716-58-3
Canonical SMILESO=C(NCCN1C(C(F)(F)F)=CC2=C1C=CC=C2)/C=C/C3=CC(OC)=C(OC)C(OC)=C3
分子式C23H23F3N2O4
分子量448.43
溶解度DMSO : ≥ 100 mg/mL (223.00 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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 uMTarget: 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 uM), except that TG6-10-1 weakly inhibited the serotonin 5-hydroxytryptamine 2B (5-HT2B) receptor with IC50 = 7.5 uM. At a high concentration (10 uM), 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.

References:
[1]. Jiang J, et al. Inhibition of the prostaglandin receptor EP2 following status epilepticus reduces delayed mortality and brain inflammation. Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-3596.