Ki16198 355025-13-7

Ki16198  355025-13-7

Ki-16198
分子式：C24H25ClN2O5S   分子量：488.98
 
产品描述
Ki16198， 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。
靶点
LPA1
LPA3
       
IC50
0.34 μM (Ki)
0.93 μM (Ki)
       
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%.
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.
溶解性
DMSO 96 mg/mL，水 <1 mg/mL，乙醇 35 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO