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Asivatrep

CAS No. 1005168-10-4

Asivatrep ( PAC-14028;PAC14028 )

Catalog No. M10042 CAS No. 1005168-10-4

Asivatrep (PAC-14028) is a potent, selective TRPV1 antagonist with IC50 of 55 nM against capsaicin-induced Ca2+ influx in rat DRG neurons.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Asivatrep
  • Note
    Research use only, not for human use.
  • Brief Description
    Asivatrep (PAC-14028) is a potent, selective TRPV1 antagonist with IC50 of 55 nM against capsaicin-induced Ca2+ influx in rat DRG neurons.
  • Description
    Asivatrep (PAC-14028) is a potent, selective TRPV1 antagonist with IC50 of 55 nM against capsaicin-induced Ca2+ influx in rat DRG neurons, does not inhibit or activate other TRP channels such as hTRPV2, hTRPV3, hTRPM8 and hTRPA1; inhibits capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations, blocks capsaicin-induced blood perfusion increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice, also attenuates dermatitis-associated barrier damages in Df and OXZ models.Dermatitis Phase 3 Clinical
  • Synonyms
    PAC-14028;PAC14028
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    TRP/TRPV Channel
  • Recptor
    TRP/TRPV Channel
  • Research Area
    Inflammation/Immunology
  • Indication
    Dermatitis

Chemical Information

  • CAS Number
    1005168-10-4
  • Formula Weight
    491.47
  • Molecular Formula
    C21H22F5N3O3S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 28 mg/mL
  • SMILES
    O=C(N[C@@H](C1=CC(F)=C(NS(=O)(C)=O)C(F)=C1)C)/C=C/C2=CC=C(C(F)(F)F)N=C2CCC
  • Chemical Name
    2-Propenamide, N-[(1R)-1-[3,5-difluoro-4-[(methylsulfonyl)amino]phenyl]ethyl]-3-[2-propyl-6-(trifluoromethyl)-3-pyridinyl]-, (2E)-

Shipping & Storage Information

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

Reference

1. Yun JW, et al. J Dermatol Sci. 2011 Apr;62(1):8-15.
2. Yun JW, et al. J Invest Dermatol. 2011 Jul;131(7):1576-9.
3. Lim KM, et al. Arch Pharm Res. 2012 Mar;35(3):393-6.
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