Molecular Formula | C24H43ClN4O3 |
Molar Mass | 471.08 |
Solubility | H2O:25mg/ml |
Storage Condition | Inert atmosphere,Room Temperature |
Use | Philanthotoxin-74, also known as PhTx-74, is a synthetic analog of the naturally-occurring wasp venom toxin philanthotoxin-4,3,3. PhTX-74 may be of potential use in studies of the neurobiological role of GluA2-containing subtypes. |
Target | IC50: 296 nM (GluR1), 296 nM (GluR1);Ki: 0.29 μM (GluR5Q) |
In vitro study | 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. |
Reference Show more | 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 |
biological activity | pharmacotoxin 74 dihydroxyzolide (PhTx 74) is an antagonist of AMPAR; the IC50 values for inhibition of GluR3 and GluR1 were 263 and 296 nM, respectively. |
Target | IC50: 296 nM (GluR1), 296 nM (GluR1) Ki: 0.29 μm (GluR5Q) |