货号	规格	价格	上海	北京	珠海	重庆	武汉
S87629-5mg买3赠1	99.80%	￥240.00 S87629-5mg ￥240.00 现货（买3赠1）	9 9	-	-	-	-
S87629-10mg促销	99.80%	￥370.00 ￥296.00 S87629-10mg ￥296.00 现货	4 4	-	-	-	-
S87629-25mg促销	99.80%	￥750.00 ￥600.00 S87629-25mg ￥600.00 现货	3 3	-	-	-	-
S87629-100mg促销	≥98%	￥2240.00 ￥1790.00 S87629-100mg ￥1790.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor

靶点：

Prostaglandin Receptor;ProstaglandinReceptor

体外研究：

TG4-155 inhibits the serotonin 5-HT2B receptor with IC50=2.6 µM and hERG (human Ether-à-go-go-Related Gene) with IC50=12 µM. PGE2 (0.1-10 μM) stimulation significantly enhances human prostate cancer cell line PC3 cell growth in a concentration-dependent manner with a maximal response being obtained at approximately 1 µM. This PGE2-induced cancer cell proliferation is significantly suppressed by TG4-155 (0.01-1μM ; 48 hours) in a concentration-dependent manner. Cell Viability Assay Cell Line: PC3 cells Concentration: 48 hours Incubation Time: 0.01, 0.1, and 1 μM Result: Significantly suppressed PGE2-induced cancer cell proliferation in a concentration-dependent manner.

体内研究：

Administration of TG4-155 (5 mg/kg, i.p.; at 1 and 12 h) significantly reduces status epilepticus (SE)-induced neurodegeneration scores in C57BL/6 mice. TG4-155 (3 mg/kg; i.p.) displays a bioavailability of 61% (i.p. route compared with i.v.), a plasma half-life (t1/2) of 0.6 h, and a brain/plasma ratio of 0.3 in C57BL/6 mice. Animal Model: C57BL/6 mice (8-12 wk old) Dosage: 5 mg/kg Administration: I.p.; at 1 and 12 h Result: Administration significantly reduced SE-induced neurodegeneration scores by 91% in hippocampal subregions CA1, by 80% in CA3, and by 63% in hilus. Animal Model: C57BL/6 mice Dosage: 3 mg/kg Administration: I.p. Result: Displayed a bioavailability of 61% (i.p. route compared with i.v.), t1/2 of 0.6 h, and a brain/plasma ratio of 0.3.

参考文献：

1. Jiang J, et al. Role of prostaglandin receptor EP2 in the regulations of cancer cell proliferation, invasion, and inflammation. J Pharmacol Exp Ther. 2013 Feb;344(2):360-7. 2. Ganesh T. Prostanoid receptor EP2 as a therapeutic target. J Med Chem. 2014 Jun 12;57(11):4454-65. 3. Jiang J, et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):3149-54.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.535 ml	12.676 ml	25.351 ml
5 mM	0.507 ml	2.535 ml	5.07 ml
10 mM	0.254 ml	1.268 ml	2.535 ml
50 mM	0.051 ml	0.254 ml	0.507 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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