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Philanthotoxin 74 dihydrochloride

CAS No. 1227301-51-0

Philanthotoxin 74 dihydrochloride( PhTx 74 dihydrochloride | PhTx-74 HCl )

Catalog No. M26786 CAS No. 1227301-51-0

Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Philanthotoxin 74 dihydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.
  • Description
    Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.(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.
  • 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.
  • In Vivo
    ——
  • Synonyms
    PhTx 74 dihydrochloride | PhTx-74 HCl
  • Pathway
    Neuroscience
  • Target
    GluR
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1227301-51-0
  • Formula Weight
    507.54
  • Molecular Formula
    C24H44Cl2N4O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (197.03 mM)
  • SMILES
    OC(C=C1)=CC=C1C[C@H](NC(CCC)=O)C(NCCCCCCCNCCCCN)=O.Cl.Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Lobachevsky PN, Vasireddy RS, Broadhurst S, Protection by methylproamine of irradiated human keratinocytes correlates with reduction of DNA damage. Int J Radiat Biol. 2011 Mar;87(3):274-83.
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