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PF-4840154

CAS No. 1332708-14-1

PF-4840154( PF-4840154 | PF 4840154 | PF4840154 )

Catalog No. M17247 CAS No. 1332708-14-1

PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel and elicited TrpA1-mediated nocifensive behaviour in mouse, with EC50 of 97 nM and 23 nM for rTrpA1 and hTrpA1, respectively.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    PF-4840154
  • Note
    Research use only, not for human use.
  • Brief Description
    PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel and elicited TrpA1-mediated nocifensive behaviour in mouse, with EC50 of 97 nM and 23 nM for rTrpA1 and hTrpA1, respectively.
  • Description
    PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models.
  • In Vitro
    ——
  • In Vivo
    PF-4840154 (30 nmol; intraplantar) elicits TrpA1-mediated nocifensive behaviour in mouse. Animal Model:Female CD1 mice (25-30g) (In TrpA1+/+ mice)Dosage:30 nmol Administration:Intraplantar (i.pl) injection Result:Elicited robust licking behavior.
  • Synonyms
    PF-4840154 | PF 4840154 | PF4840154
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    rTRPA1|hTRPA1
  • Research Area
    Inflammation/Immunology
  • Indication
    ——

Chemical Information

  • CAS Number
    1332708-14-1
  • Formula Weight
    466.63
  • Molecular Formula
    C26H38N6O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 50 mg/mL. 107.15 mM;
  • SMILES
    CC(C)CNc2nc(ncc2C(=O)NCc1ccccc1)N3CCN(CC3)CC4CCCOC4
  • Chemical Name
    N-benzyl-4-(2-methylpropylamino)-2-[4-(oxan-3-ylmethyl)piperazin-1-yl] pyrimidine-5-carboxamide

Shipping & Storage Information

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

Reference

1.Ryckmans T,etal.Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel.Bioorg Med Chem Lett. 2011 Aug 15;21(16):4857-9.
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