Philanthotoxin 74 dihydrochloride

SKU: orb1307882

Description

Philanthotoxin 74 dihydrochloride is a selective AMPA receptor antagonist, exhibiting potent inhibitory activity against GluR1 and GluR3 subunits with IC50 values in the nanomolar range. This tool compound is widely used in neuroscience research to investigate glutamatergic signaling, synaptic plasticity, and excitotoxicity in both cellular and animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1227301-51-0
• MW: 507.54
• Purity: 99.75%
• Formula: C₂₄H₄₄Cl₂N₄O₃
• SMILES: OC(C=C1)=CC=C1C[C@H](NC(CCC)=O)C(NCCCCCCCNCCCCN)=O.Cl.Cl
• Target: iGluR,GluR
• Solubility: H2O:40 mg/mL (78.81 mM);DMSO:90 mg/mL (177.33 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.5 mM)

Bioactivity

• Target IC50:
  GluR1:296 nM
• In Vitro:
  Philanthotoxin 74 dihydrochloride inhibits the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3 in the micromolar concentration range, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 dihydrochloride (500 μM) fully inhibits GluA1/A2R receptors and produces 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74 dihydrochloride (100 and 500 μM) displays a pronounced channel block (> 80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Philanthotoxin 74 dihydrochloride inhibits these receptors nonselectively, with IC50 values of about 30 μM, in both the presence and absence of γ-2.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GluR3, GluR1, GluR5, AMPAR, PhTx 74, PhTx 74 dihydrochloride, PhTx 74 Dihydrochloride, PhTx-74 HCl, Philanthotoxin 74, Philanthotoxin 74 Dihydrochloride

Compound Identifiers

PubChem CID

46213501