1393814-38-4

1393814-38-4 structure

Name: TC LPA5 4
Chemical Name: 5-(3-chloro-4-cyclohexylphenyl)-1-(3-methoxyphenyl)-1H-pyrazole-3-carboxylic acid
CAS Number: 1393814-38-4
Molecular Formula: C₂₃H₂₃ClN₂O₃
Molecular Weight: 410.89
Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
Create Date: 2016-12-11 12:07:55
Modify Date: 2024-01-02 22:17:33
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].

Name	5-(3-chloro-4-cyclohexylphenyl)-1-(3-methoxyphenyl)-1H-pyrazole-3-carboxylic acid

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> LPL Receptor
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]. Animal Model: BALB/C nu/nu mice, aged 4 5 weeks (CGTH-W3 xenografts) [2] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 5 days/week for 2 weeks Result: Significantly inhibits CGTH-W3 xenograft growth with inhibitory rates of 46.7%.
References	[1]. Kozian DH, et al. Selective non-lipid modulator of LPA5 activity in human platelets. Bioorg Med Chem Lett. 2012;22(16):5239-5243. [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.

Molecular Formula	C₂₃H₂₃ClN₂O₃
Molecular Weight	410.89
Exact Mass	410.14000
PSA	64.35000
LogP	5.94720

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