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 agent targets^[1]. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells^[2].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TC LPA5 4 (10 mg/kg; intraperitoneal injection; 5 days/week for 2 weeks) could delay CGTH-W3 xenograft growth in nude mice^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

410.89

Solid

C₂₃H₂₃ClN₂O₃

1393814-38-4

O=C(C1=NN(C2=CC=CC(OC)=C2)C(C3=CC=C(C4CCCCC4)C(Cl)=C3)=C1)O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Kozian DH, et al. Selective non-lipid modulator of LPA5 activity in human platelets. Bioorg Med Chem Lett. 2012;22(16):5239-5243.  [Content Brief]

  [2]. Zhao WJ, et al. LPAR5 promotes thyroid carcinoma cell proliferation and migration by activating class IA PI3K catalytic subunit p110β. Cancer Sci. 2021;112(4):1624-1632.  [Content Brief]