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Philanthotoxin 74
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Philanthotoxin 74图片
CAS NO:1227301-51-0
包装与价格:
包装价格(元)
1mg电议
10mg电议
50mg电议

产品介绍
Philanthotoxin 74 (PhTx 74) 是一种 AMPAR 拮抗剂;抑制 GluR3 和 GluR1,IC50 分别为 263 和 296 nM。
Cas No.1227301-51-0
别名PhTx 74 dihydrochloride
化学名(S)-N-(1-((7-((4-aminobutyl)amino)heptyl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)butyramide dihydrochloride
Canonical SMILESO=C([C@H](CC(C=C1)=CC=C1O)NC(CCC)=O)NCCCCCCCNCCCCN.Cl.Cl
分子式C24H42N4O3.2HCl
分子量507.54
溶解度DMSO: 100 mM,Water: 100 mM
储存条件Desiccate at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.

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].

References:
[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.