中文名 | Philanthotoxin 74 |
英文名 | (S)-N-(1-((7-((4-aminobutyl)amino)heptyl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)butyramide dihydrochloride |
别名 | 化合物 T16524 |
英文别名 | PhTx-74 diHCl Philanthotoxin 74 PhTx-74 dihydrochloride Philanthotoxin 74 (hydrochloride) Philanthotoxin 74 dihydrochloride (S)-N-(1-((7-((4-aminobutyl)amino)heptyl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)butyramide dihydrochloride |
CAS | 1227301-51-0 |
化学式 | C24H43ClN4O3 |
分子量 | 471.08 |
溶解度 | H2O:25 mg/ml |
存储条件 | Inert atmosphere,Room Temperature |
靶点 | IC50: 296 nM (GluR1), 296 nM (GluR1);Ki: 0.29 μM (GluR5Q) |
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 IC 50 values of about 30 μM, in both the presence and absence of γ-2. |
参考资料 展开查看 | 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. |
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 |
5 mM | 0.039 ml | 0.197 ml | 0.394 ml |
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