Philanthotoxin 74 dihydrochloride

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

Product information

CAS Number: 1227301-51-0

Molecular Weight: 507.54

Formula: C24H44Cl2N4O3

Chemical Name: N-[(1S)-1-({7-[(4-aminobutyl)amino]heptyl}carbamoyl)-2-(4-hydroxyphenyl)ethyl]butanamide dihydrochloride

Smiles: Cl.Cl.CCCC(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)NCCCCCCCNCCCCN

InChiKey: HWTJQQMIKVJWLH-IKXQUJFKSA-N

InChi: InChI=1S/C24H42N4O3.2ClH/c1-2-10-23(30)28-22(19-20-11-13-21(29)14-12-20)24(31)27-18-8-5-3-4-7-16-26-17-9-6-15-25;;/h11-14,22,26,29H,2-10,15-19,25H2,1H3,(H,27,31)(H,28,30);2*1H/t22-;;/m0../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (197.03 mM; Need ultrasonic). H2O : 50 mg/mL (98.51 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

Products are for research use only. Not for human use.