Philanthotoxin 74 dihydrochloride 是一种 AMPAR 拮抗剂,对 GluR3 和 GluR1 的 IC50 分别为 263 和 296 nM。
产品描述
Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.
体外活性
Philanthotoxin 74 dihydrochloride inhibits the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3 in the micromolar concentration range, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 dihydrochloride (500 μM) fully inhibits GluA1/A2R receptors and produces 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74 dihydrochloride (100 and 500 μM) displays a pronounced channel block (>80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Philanthotoxin 74 dihydrochloride inhibits these receptors nonselectively, with IC50 values of about 30 μM, in both the presence and absence of γ-2[1].
Cas No.
1227301-51-0
分子式
C24H44Cl2N4O3
分子量
507.54
别名
PhTx 74 dihydrochloride
储存和溶解度
DMSO:90 mg/mL (177.33 mM),Need ultrasonic
H2O:40 mg/mL (78.81 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years