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 selectiveEP2 receptorantagonist with aKiof 9.9 nM[1][2]. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1[1]. TG4-155 has an EP2 Schild KBof 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 andIP, but only 14-fold selectivity against the DP1 receptor[2]. |
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].
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. |
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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].
| 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.), t1/2of 0.6 h, and a brain/plasma ratio of 0.3. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(316.89 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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
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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。 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本网站选购。
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