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Philanthotoxin 74 (hydrochloride)

  Cat. No.:  DC10763   Featured
Chemical Structure
1227301-51-0
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Field of application
Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1227301-51-0
Chemical Name: N-[7-[(4-aminobutyl)amino]heptyl]-4-hydroxy-αS-[(1-oxobutyl)amino]-benzenepropanamide, dihydrochloride
Synonyms: PhTx 74 dihydrochloride
SMILES: O=C(NCCCCCCCNCCCCN)[C@@H](NC(CCC)=O)CC1=CC=C(O)C=C1.[H]Cl.[H]Cl
Formula: C24H42N4O3.2HCl
M.Wt: 507.5
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
Target: IC50: 296 nM (GluR1), 296 nM (GluR1)[1] Ki: 0.29 μM (GluR5Q)[2]
In Vitro: 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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