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TC LPA5 4
LPA5受体拮抗剂,LPA5-IN-4 is the first non-lipid, small-molecule inhibitor for LPA5/GPR92, specifically inhibiting LPA-mediated platelet activation in vitro.
目录号: PC11017 纯度: ≥98%
CAS No. :1393814-38-4
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Medlife所售产品仅用于科学研究(非临床研究),非药品不可食用,不可用于人体或动物的临床诊断和治疗,我们不为个人提供产品及服务。产品COA等资料,可至下方“质量控制”中下载。
中文名称
TC LPA5 4
英文名称
TC LPA5 4
英文别名
TC LPA5 4;5-(3-chloro-4-cyclohexylphenyl)-1-(3-methoxyphenyl)-1H-pyrazole-3-carboxylic acid
Cas No.
1393814-38-4
分子式
C23N2O3ClH23
分子量
410.89
包装储存

4°C, protect from light

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

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. TC LPA5 4 inhibits cell proliferation and migration of thyroid cancer cells.

性状

Solid

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.

Medlife 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.

Medlife 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)
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%.
运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

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

参考文献
溶解度数据
体外研究: 

DMSO : 62.5 mg/mL (152.11 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4337 mL 12.1687 mL 24.3374 mL
5 mM 0.4867 mL 2.4337 mL 4.8675 mL
10 mM 0.2434 mL 1.2169 mL 2.4337 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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