Ki 16425 (Ki16425)是竞争性的溶血磷脂酸受体(LPA)亚型可逆的选择性拮抗剂,作用于LPA1/2/3的Ki值为0.34 μM,6.5 μM和0.93 μM,对LPA4/5/6无明显活性。Ki16425按照LPA1 ≥LPA3 >> LPA2的递减顺序抑制LPA诱导的反应,抑制LPA诱导的鸟苷5'-O-(3-硫代三磷酸)结合和膜成分结合,还抑制LPA 诱导的长期反应,包括DNA合成和细胞迁移。
参考文献
[1] Ohta H, et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.Mol Pharmacol. 2003 Oct;64(4):994-1005.
[2] Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012 Aug 17;150(4):780-91.
[3] Ma L, et al. Evidence for lysophosphatidic acid 1 receptor signaling in the early phase of neuropathic pain mechanisms in experiments using Ki-16425, a lysophosphatidic acid 1 receptor antagonist. J Neurochem. 2009 Apr;109(2):603-10.
冰袋运输。粉末直接保存于-25~-15℃,有效期3年。建议分装后-25~-15℃干燥保存,避免反复冻融。