Ki16198

Ki16198CAS号: 355025-13-7分子式: C24H25ClN2O5S分子量: 488.98描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

Ki16198是Ki16425的甲酯,是LPA拮抗剂,抑制LPA1-和LPA3诱导的肌醇磷酸产生,Ki分别为0.34 μM和0.93 μM,对LPA2具有较弱的抑制作用,对LPA4, LPA5, LPA6没有抑制活性。Ki16198或Ki16425充分抑制LPA1和LPA3介导的反应,具有相似的效力,对LPA2具有低的作用效果,对LPA4, LPA5和LPA6没有抑制活性。Ki16198(10 μM)作用于 YAPC-PD癌细胞,有效抑制响应LPA的迁移和入侵,与Ki16425具有相似的效力。Ki16198(10 μM)作用于YAPC-PD细胞,抑制LPA诱导的proMMP-9蛋白和mRNA表达。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
3-[[[4-[4-[[[1-(2-氯苯基)乙氧基]羰基]氨基]-3-甲基-5-异恶唑基]苯基]甲基]硫基]-丙酸甲酯
可溶性/溶解性
DMSO :96 mg/mL (196.32 mM)

Ethanol :35 mg/mL (71.57 mM)

生物活性
靶点
LPA1,LPA3
In vitro(体外研究)
Ki16198 or Ki16425 substantially inhibits LPA1- and LPA3-mediated responses with a similar potency, with low potency to LPA2 and no activity to LPA4, LPA5 and LPA6. Ki16198 (10 μM) is also effective to inhibit migration and invasion responses to LPA in YAPC-PD cancer cell line with a potency similar to that of Ki16425. Ki16198 (10 μM) inhibits the LPA-induced expression of proMMP-9 protein and mRNA in YAPC-PD cells. Ki16198 (1 μM) inhibits the proliferation of lpa1Δ-1 and lpa1Δ+-1 cells by about 70%.
In vivo(体内研究)
Ki16198 (2 mg/kg) significantly decreases the total metastatic node weight in the peritoneal cavity and ascites formation by 50% in YAPC-PD xenograft mouse model. Ki16198 (60 mg/kg orally) significantly inhibits lactate-induced limb lesions in rats.

分子结构图

Ki16198