TC LPA5 4

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TC LPA5 4 

TC LPA5 4 是一种特异性非脂质 LPA5 (GPR92) 拮抗剂。TC LPA5 4 抑制 LPA 诱导的离体人血小板 (LPA5-RH7777细胞系) 聚集,IC50 为 800 nM。TC LPA5 4 对 LPA5 的选择性超过 80 个其他筛选药物靶点。TC LPA5 4 抑制甲状腺癌细胞的增殖和迁移。

TC LPA5 4

TC LPA5 4 Chemical Structure

CAS No. : 1393814-38-4

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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%.

分子量

410.89

Formula

C23H23ClN2O3

CAS 号

1393814-38-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

发表评论