TG4-155

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TG4-155  纯度: 99.69%

TG4-155 是一种有效的脑渗透性的选择性 EP2 受体拮抗剂，Ki 为 9.9 nM。TG4-155 只对 EP2 和 DP1 具有低纳摩尔的拮抗活性。TG4-155 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。

TG4-155

TG4-155 Chemical Structure

CAS No. : 1164462-05-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥990 In-stock
5 mg ￥900 In-stock
10 mg ￥1500 In-stock
25 mg ￥3000 In-stock
50 mg ￥5200 In-stock
100 mg ￥9100 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. 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[2].

IC50 & Target

EP2 Receptor

9.9 nM (Ki)

体外研究
(In Vitro)

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[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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
(In Vivo)

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[3].
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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (8-12 wk old)[3]
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[3]
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.

分子量

394.46

Formula

C23H26N2O4
CAS 号

1164462-05-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (316.89 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5351 mL 12.6756 mL 25.3511 mL
5 mM 0.5070 mL 2.5351 mL 5.0702 mL
10 mM 0.2535 mL 1.2676 mL 2.5351 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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