| 产品描述: | LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high brain permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research. LPA5 antagonist 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. |
| 体外研究: |
LPA5 antagonist 2 (0-10 μM) inhibits hLPA5 calcium mobilization with an IC50 value of 32 nM. LPA5 antagonist 2 (0-10 μM) shows good target selectivity for LPA5. |
| 体内研究: |
LPA5 antagonist 1 (intraperitoneal injection; 17.8 mg/kg; once) treatment shows good brain exposure in vivo. LPA5 antagonist 1 (intraperitoneal injection; 5.6, 10, and 17.8 mg/kg; once) treatment reduces mechanical allodynia in inflammatory pain model. |
| 参考文献: |
1. Zhang DH, et al. Isoquinolone derivatives as lysophosphatidic acid receptor 5 (LPA5) antagonists: Investigation of structure-activity relationships, ADME properties and analgesic effects. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. Volume 243, 5 December |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.055 ml |
10.276 ml |
20.552 ml |
| 5 mM |
0.411 ml |
2.055 ml |
4.11 ml |
| 10 mM |
0.206 ml |
1.028 ml |
2.055 ml |
| 50 mM |
0.041 ml |
0.206 ml |
0.411 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。 |