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TG4-155
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。
TG4-155图片
CAS NO:1164462-05-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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。

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

体外活性

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[1].

体内活性

TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine. It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost[2].

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].

Cas No.

1164462-05-8

分子式

C23H26N2O4

分子量

394.471

储存和溶解度

DMSO:125 mg/mL (316.89 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years