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Pico145

CAS No. 1628287-16-0

Pico145( HC-608 )

Catalog No. M23723 CAS No. 1628287-16-0

Pico145 is a remarkable inhibitor of TRPC1/4/5 channels. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Pico145
  • Note
    Research use only, not for human use.
  • Brief Description
    Pico145 is a remarkable inhibitor of TRPC1/4/5 channels. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels.
  • Description
    Pico145 is a remarkable inhibitor of TRPC1/4/5 channels. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells) It also shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.
  • In Vitro
    Pico145 (Compound 31, C31) is a remarkable small-molecule inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells; Pico145 shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers expressed in HEK 293 Tet+ cells (IC50, 0.03 nM and 0.2 nM, respectively). The potency of Pico145 can be reduced by increased (?)-englerin A concentration. Furthermore, Pico145 potently inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P), and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels with an IC50 of 0.011 nM. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC50, 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca2+ entry and histamine-evoked Ca2+ entry into endothelial cells.
  • In Vivo
    ——
  • Synonyms
    HC-608
  • Pathway
    Membrane Transporter/Ion Channel
  • Target
    TRP/TRPV Channel
  • Recptor
    TRPC4, cell assay|TRPC5, cell assay|TRPC4-TRPC1, cell assay|TRPC5-TRPC1, cell assay
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1628287-16-0
  • Formula Weight
    524.88
  • Molecular Formula
    C23H20ClF3N4O5
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 99 mg/mL (188.61 mM)
  • SMILES
    CN(c1c(C(N2CCCO)=O)n(Cc(cc3)ccc3Cl)c(Oc3cc(OC(F)(F)F)ccc3)n1)C2=O
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Rubaiy HN, et al. Picomolar, selective, and subtype-specific small-molecule inhibition of TRPC1/4/5 channels. J Biol Chem. 2017 May 19;292(20):8158-8173.
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