| 产品描述: | LPA1和LPA3受体拮抗剂;LPA1and LPA3receptor antagonist;Ki16425是竞争性的可逆的LPA拮抗剂,对LPA1,LPA2和LPA3的Ki分别为0.34 μM,6.5 μM和0.93 μM,而对LPA4,LPA5和LPA6无活性。;Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM in RH7777 cell lines, respectively, shows no activity at LPA4, LPA5, LPA6.A competitive inhibitor of EDG-2, EDG-4, and EDG-7. |
| 体内研究: |
Ki16425 (Debio 0719) (1-30 mg/kg;腹腔注射;在注射 LPA 前 30 分钟) 可抑制 LPA 诱发的神经性疼痛样行为。 |
| 参考文献: |
1. Ohta H, et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.Mol Pharmacol, 2003, 64(4), 994-1005. 2. Moughal NA, et al. Protean agonism of the lysophosphatidic acid receptor-1 with Ki16425 reduces nerve growth factor-induced neurite outgrowth in pheochromocytoma 12 cells. J Neurochem, 2006, 98(6), 1920-1929. 3. Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012 Aug 17;150(4):780-91. 4. 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, 109(2), 603-610. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.105 ml |
10.527 ml |
21.054 ml |
| 5 mM |
0.421 ml |
2.105 ml |
4.211 ml |
| 10 mM |
0.211 ml |
1.053 ml |
2.105 ml |
| 50 mM |
0.042 ml |
0.211 ml |
0.421 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |