| 产品描述： | Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively. |
| 靶点： |
IC50: 296 nM (GluR1), 296 nM (GluR1);Ki: 0.29 μM (GluR5Q);GluR; iGluR |
| 体外研究： |
Philanthotoxin 74 in the micromolar concentration range displays selective inhibition between the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 is reported to fully inhibit GluA1/A2R receptors when applied at a concentration of 500 μM while producing 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74, when tested at concentrations of 100 and 500 μM, displays pronounced channel block (more than 80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Oocytes expressing GluA2R alone that homomeric GluA2R is virtually inert to philanthotoxin 74 in the 0.1-300 μM concentration range, displaying less than 5% inhibition at the maximum tested concentration of 300 μM. Philanthotoxin 74 inhibits these receptors nonselectively, with IC50 values of about 30 μM, in both the presence and absence of γ-2. |
| 参考文献： |
1. Poulsen MH, et al. Evaluation of PhTX-74 as subtype-selective inhibitor of GluA2-containing AMPA receptors. Mol Pharmacol. 2014 Feb;85(2):261-8.2. Kromann H, et al. Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors. J Med Chem. 2002 Dec 19;45(26):5745-54. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ 氮气保存 |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.97 ml |
9.851 ml |
19.703 ml |
| 5 mM |
0.394 ml |
1.97 ml |
3.941 ml |
| 10 mM |
0.197 ml |
0.985 ml |
1.97 ml |
| 50 mM |
0.039 ml |
0.197 ml |
0.394 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京