DC Chemicals Limited
China
Product Name: Philanthotoxin 74 (hydrochloride)
Price: $650.0/100mg $1100.0/250mg $2250.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1227301-51-0

1227301-51-0 structure

Name: Philanthotoxin 74
Chemical Name: N-{7-[(4-Aminobutyl)amino]heptyl}-Nα-butyryltyrosinamide dihydrochloride
CAS Number: 1227301-51-0
Molecular Formula: C₂₄H₄₄Cl₂N₄O₃
Molecular Weight: 507.537
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2018-01-18 05:07:27
Modify Date: 2024-01-16 12:10:23
Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.

Name	N-{7-[(4-Aminobutyl)amino]heptyl}-Nα-butyryltyrosinamide dihydrochloride
Synonyms	N-{7-[(4-Aminobutyl)amino]heptyl}-Nα-butyryltyrosinamide dihydrochloride Benzenepropanamide, N-[7-[(4-aminobutyl)amino]heptyl]-4-hydroxy-α-[(1-oxobutyl)amino]-, (αS)-, hydrochloride (1:2) Philanthotoxin 74 dihydrochloride

Description	Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR Signaling Pathways >> Neuronal Signaling >> iGluR Research Areas >> Neurological Disease
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.

Molecular Formula	C₂₄H₄₄Cl₂N₄O₃
Molecular Weight	507.537
Exact Mass	506.279053
Storage condition	2-8℃

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