Philanthotoxin 74 dihydrochloride,1227301-51-0

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YZ剂描述：

产品名称：Philanthotoxin 74 dihydrochloride

产品别名：PhTx 74 dihydrochloride

英文别名：PhTx 74 dihydrochloride

靶点：iGluR

CAS：1227301-51-0

纯度：98%

外观：A white to off-white solid

保存方法：-20°C

描述：

 Philanthotoxin 74 dihydrochloride (PhTx 74) 是 AMPAR 的拮抗剂; YZ GluR3 和 GluR1 的 IC50 值分别为263和296 nM。

溶解性：Soluble in DMSO > 10 mM

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.

体内研究：

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