TG4-155,99.69%

产品编号:Bellancom-18971| CAS NO:1164462-05-8| 分子式:C23H26N2O4| 分子量:394.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-18971
900.00 杭州 北京(现货)
Bellancom-18971
1500.00 杭州 北京(现货)
Bellancom-18971
3000.00 杭州 北京(现货)
Bellancom-18971
5200.00 杭州 北京(现货)
Bellancom-18971
9100.00 杭州 北京(现货)

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TG4-155

产品介绍 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。
生物活性

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
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 西域 网站选购。
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
参考文献

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