Philanthotoxin 74 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Philanthotoxin 74 diHClide 是 AMPAR 的拮抗剂，对 GluR3 和 GluR1 的 IC50 分别为 263 和 296 nM。

Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.(In Vitro):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.

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.

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PhTx 74 dihydrochloride | PhTx-74 HCl

Neuroscience

GluR

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1227301-51-0

507.54

C24H44Cl2N4O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (197.03 mM)

OC(C=C1)=CC=C1C[C@H](NC(CCC)=O)C(NCCCCCCCNCCCCN)=O.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years