TC LPA5 4是一种特异性非脂质 LPA5 (GPR92) 拮抗剂,能够抑制 LPA 诱导的人血小板 (LPA5-RH7777 细胞系) 聚集 (IC50 = 800 nM),并对超过 80 种其他分子靶点显示出高选择性,抑制甲状腺癌细胞的增殖和迁移。
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描述 | TC LPA5 4 is an LPA5 (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibited LPA-induced aggregation of isolated human platelets (LPA5-RH7777 cell line) with an IC50 of 800 nM. TC LPA5 4 showed selectivity for LPA5 among 80 targets screened[1].TC LPA5 4 significantly inhibited the proliferation of thyroid cancer cells CGTH-W3, TPC-1, B-CAPAP and BHT101, with IC50s of 103.0 μM, 84.9 μM, 55.9 μM and 57.17 μM, respectively. At concentration of 5 μM for 24 hours, TC LPA5 4 significantly inhibited the migration of CGTH-W3 and TPC-1 cells stimulated by LPA, with an inhibition rate of about 30%. As B-CPAP and BHT101 cells expressed higher LPAR5 mRNA, TC LPA5 4 inhibited the proliferation of these two cell lines, with IC50s of 55.9 μM and 57.17 μM, whereas, as CGTH-W3 and TPC-1 cells expressed lower LPAR5 mRNA, TC LPA5 4 had different anti-tumour activities, with IC50s of 103.0 μM and 84.9 μM, respectively[2]. |
Animal study | At a dose of 10 mg/kg administered intraperitoneally for 5 days/week for 2 weeks, TC LPA5 4 delayed the growth of CGTH-W3 xenograft nude mice with an inhibition rate of 46.7%[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.43mL 0.49mL 0.24mL |
12.17mL 2.43mL 1.22mL |
24.34mL 4.87mL 2.43mL |
CAS号 | 1393814-38-4 |
分子式 | C23H23ClN2O3 |
分子量 | 410.893 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 60 mg/mL(146.02 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 |
动物实验配方 |