生物活性 | |||
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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]. |
实验方案 | |||
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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 |
参考文献 |
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