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Pyr6

CAS No. 245747-08-4

Pyr6 ( N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide )

Catalog No. M22852 CAS No. 245747-08-4

Pyr6 is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.Pyr3 is selective inhibitor of TRPC3, inhibited Orai1- and TRPC3-mediated Ca(2+) entry and currents as well as mast cell activation with similar potency.?

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Pyr6
  • Note
    Research use only, not for human use.
  • Brief Description
    Pyr6 is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.Pyr3 is selective inhibitor of TRPC3, inhibited Orai1- and TRPC3-mediated Ca(2+) entry and currents as well as mast cell activation with similar potency.?
  • Description
    Pyr6 is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.Pyr3 is selective inhibitor of TRPC3, inhibited Orai1- and TRPC3-mediated Ca(2+) entry and currents as well as mast cell activation with similar potency.?By contrast, Pyr6 exhibited a 37-fold higher potency to inhibit Orai1-mediated Ca(2+) entry as compared with TRPC3-mediated Ca(2+) entry and potently suppressed mast cell activation.
  • Synonyms
    N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    TRP/TRPV Channel
  • Recptor
    TRPC3
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    245747-08-4
  • Formula Weight
    418.27
  • Molecular Formula
    C17H9F7N4O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:95 mg/mL (227.12 mM)
  • SMILES
    O=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-22.
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