TC LPA5 4

TC LPA5 4 is a LPA₅ (GPR92)-specific non-lipid antagonist. TC LPA5 4 inhibits LPA-induced aggregation of isolated human platelet (LPA₅-RH7777 cell line) with an IC₅₀ of 800 nM. TC LPA5 4 displays selectivity for LPA₅ over 80 other screened drug targets^[1]. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells^[2]. In Vitro: TC LPA5 4 inhibits the proliferation on thyroid cancer cells CGTH-W3, TPC-1, B-CAPAP, and BHT101 significantly with IC₅₀ at 103.0 μM, 84.9 μM, 55.9μM, and 57.17 μM. TC LPA5 4 (5 μM; 24 hours) significantly inhibits LPA-stimulated migration of CGTH-W3 and TPC-1 cells, with an inhibitory rate of ~ 30%. B-CPAP and BHT101 cells expressed higher LPAR5 mRNA. TC LPA5 4 inhibits these two cell lines’ proliferations with IC₅₀ at 55.9μM and 57.17 μM. CGTH-W3 and TPC-1 cells expressed lower LPAR5 mRNA. TC LPA5 4 displays differential antitumor activity with IC₅₀ at 103.0 μM and 84.9 μM^[2]. In Vivo: TC LPA5 4 (10 mg/kg; intraperitoneal injection; 5 days/week for 2 weeks) could delay CGTH-W3 xenograft growth in nude mice^[2].