TG4-155是一种有效的穿脑选择性EP2受体拮抗剂,其Ki为9.9 nM。TG4-155仅对EP2和DP1受体显示低纳摩尔级别的拮抗活性。TG4-155对EP2的KB为2.4 nM,显示出对DP1受体的14倍选择性,对EP1、EP3、EP4和IP受体的选择性为550-4750倍。
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Concentration | Treated Time | Description | References | |
C6G cells | 10 µM | 2 days | To evaluate the cytotoxicity of TG4-155, results showed that TG4-155 had no significant cytotoxicity at 10 μM. | J Pharmacol Exp Ther. 2013 Feb;344(2):360-7. |
PC3 cells | 1 µM | 24 hours | To evaluate the effect of TG4-155 on PC3 cell invasion, results showed that TG4-155 completely prevented butaprost-induced cell invasion. | J Pharmacol Exp Ther. 2013 Feb;344(2):360-7. |
SH-SY5Y cells | 20 µM | 24 hours | To evaluate the protective effect of TG4-155 on 6-OHDA-induced cytotoxicity, results showed that TG4-155 significantly reduced 6-OHDA-induced cytotoxicity. | Sci Rep. 2017 Aug 25;7(1):9459. |
Neuro-2a cells | 10 or 20 µM | 24 hours | To evaluate the protective effect of TG4-155 on 6-OHDA-induced cytotoxicity, results showed that TG4-155 significantly reduced 6-OHDA-induced cytotoxicity. | Sci Rep. 2017 Aug 25;7(1):9459. |
PC3 cells | 1 µM | 48 hours | To evaluate the effect of TG4-155 on PC3 cell proliferation, results showed that TG4-155 significantly inhibited PGE2- or butaprost-induced cell proliferation. | J Pharmacol Exp Ther. 2013 Feb;344(2):360-7. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.54mL 0.51mL 0.25mL |
12.68mL 2.54mL 1.27mL |
25.35mL 5.07mL 2.54mL |
CAS号 | 1164462-05-8 |
分子式 | C23H26N2O4 |
分子量 | 394.46 |
SMILES Code | CC1=CC2=C(C=CC=C2)N1CCNC(/C=C/C3=CC(OC)=C(C(OC)=C3)OC)=O |
MDL No. | MFCD03829939 |
别名 | |
运输 | 蓝冰 |
InChI Key | YBHUXHFZLMFETJ-MDZDMXLPSA-N |
Pubchem ID | 5886965 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 120 mg/mL(304.21 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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