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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-TG6-10-1
TG6-10-1

Chemical Structure : TG6-10-1

CAS No.: 1415716-58-3

TG6-10-1 (EP2 antagonist)

货号: PC-45111Not For Human Use, Lab Use Only.

TG6-10-1 is a potent and selective antagonist of prostaglandin E2 receptor subtype EP2 with Kb of 17.8 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TG6-10-1 is a potent and selective antagonist of prostaglandin E2 receptor subtype EP2 with Kb of 17.8 nM.
TG6-10-1 displays >300-fold selectivity over EP3, EP4, and IP receptors, 100-fold selectivity over EP1, 25-fold selectivity over FP and TP, and 10-fold selectivity over DP1 receptors.
TG6-10-1 completely recapitulates the effects of conditional ablation of COX-2 from principal forebrain neurons, accelerates recovery from weight loss, reduces brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus, without modifying seizures acutely in the mouse pilocarpine model of SE.

物理化学性质&存储条件

分子量 448.4349
分子式 C23H23F3N2O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Propenamide, N-[2-[2-(trifluoromethyl)-1H-indol-1-yl]ethyl]-3-(3,4,5-trimethoxyphenyl)-, (2E)-

参考文献

1. Jiang J, et al. Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-6.

2. Rojas A, et al. Neuropharmacology. 2015 Jun;93:15-27.

3. Rojas A, et al. Neuropharmacology. 2016 Nov;110(Pt A):419-30.

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