TG4-155

产品编号 T5482Cas号 1164462-05-8

TG4-155 是一种脑渗透性 EP2 拮抗剂，对 EP2 和 DP1 具有低纳摩尔的拮抗活性。它作用于 EP2 的 KB 为 2.4 nM，比对 DP1 受体的选择性高 14 倍，比对 EP1、EP3、EP4 和 IP 的选择性比高 550-4750 倍。

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TG4-155

产品编号 T5482Cas号 1164462-05-8

规格	价格	库存
1 mg	¥ 297	现货
2 mg	¥ 433	现货
5 mg	¥ 739	现货
10 mg	¥ 1,230	现货
25 mg	¥ 2,490	现货
50 mg	¥ 3,730	现货
100 mg	¥ 5,380	现货
1 mL x 10 mM (in DMSO)	¥ 815	现货

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产品介绍

生物活性

产品描述	TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 μM) and a panel of other receptors and channels
靶点活性	EP2 receptor:9.9 nM (Ki)
体外活性	TG4-155是一种能穿透大脑的EP2拮抗剂（KB=2.4 nM），其对EP4的效果降低超过1000倍（KB=11.4 μM），并且对一系列其他受体和通道[1]的作用也较低。
体内活性	TG4-155在由山梨醇引发的癫痫持续状态小鼠模型中显著减少神经退行性变化。该化合物抑制了经布他前列素[2]处理的癌细胞中的增殖、侵袭及炎症细胞因子表达。
细胞实验	Cytotoxicity of TG4-155 was examined with the CellTiter-Glo Luminescent Cell Viability Assay by measuring cellular ATP level, which correlates with cell viability.?Briefly, C6G cells were plated in 384-well plates at 2,000 cells/well in 25 μl DMEM plus test compound and incubated for 2 days.?CellTiter-Glo reagent (25 μl) was then added to each well.?The contents were mixed for 2 minutes on an orbital shaker to induce cell lysis and incubated at room temperature for 10 minutes.?Relative viability is proportional to luminescence intensity as measured by a microplate reader with an integration time of 1 second[2].
动物实验	C57BL/6 mice (8 12 wk old) were injected with pilocarpine (280 mg/kg, i.p.) to induce status epilepticus (SE). SE was allowed for 1 h and terminated by pentobarbital (30 mg/kg, i.p.). Mice were then randomized by assignment to a random number stream and received two doses of vehicle or TG4-155 (5 mg/kg, i.p.) at 1 and 12 h after SE termination. Mice were euthanized under deep isoflurane anesthesia 24 h after SE and brains were collected for histology[1].

化学信息

分子量	394.46
分子式	C₂₃H₂₆N₂O₄
CAS No.	1164462-05-8

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 125 mg/mL (316.89 mM)

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5351 mL	12.6756 mL	25.3511 mL	126.7556 mL
5 mM	0.5070 mL	2.5351 mL	5.0702 mL	25.3511 mL
10 mM	0.2535 mL	1.2676 mL	2.5351 mL	12.6756 mL
20 mM	0.1268 mL	0.6338 mL	1.2676 mL	6.3378 mL
50 mM	0.0507 mL	0.2535 mL	0.5070 mL	2.5351 mL
100 mM	0.0254 mL	0.1268 mL	0.2535 mL	1.2676 mL