Philanthotoxin 74 dihydrochloride

Cat. No. :	HY-104020A
M.Wt:	507.54
Formula:	C24H44Cl2N4O3
Purity:	>98 %
Solubility:	DMSO : 100 mg/mL (ultrasonic);H2O : 50 mg/mL (ultrasonic)

Introduction of 1227301-51-0 :

Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC₅₀s of 263 and 296 nM, respectively^[1][2]. IC50 & Target:IC50: 296 nM (GluR1), 296 nM (GluR1)^[1]

Ki: 0.29 μM (GluR5Q)^[2]

In Vitro: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^[1].