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Philanthotoxin 74 Sale

(Synonyms: PhTx 74 dihydrochloride) 目录号 : GC12703

An AMPA receptor antagonist

Philanthotoxin 74 Chemical Structure

Cas No.:1227301-51-0

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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.

Chemical Properties

Cas No. 1227301-51-0 SDF
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 SMILES O=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
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1 mM 1.9703 mL 9.8514 mL 19.7029 mL
5 mM 0.3941 mL 1.9703 mL 3.9406 mL
10 mM 0.197 mL 0.9851 mL 1.9703 mL
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