Catalog Number: 2006
Chemical Name: (2R,4bS,6aS,12bS,12cR,14aS)-5,6,6a,7,12,12b,12c,13,14,14a-Decahydro-4b-hydroxy-2-(1-hydroxy-1-methylethyl)-12b,12c-dimethyl-2H-pyrano[2'',3'':5',6']benz[1',2':6,7]indeno[1,2-b]indol-3(4bH)-one
Biological Activity
Potent blocker of high-conductance Ca2+-activated K+ (BKCa, KCa1.1) channels. Binds to the α-subunit of BKCa (Ki = 1.9 nM for block of currents in α-subunit-expressing oocytes) and enhances binding of charybdotoxin to BKCa channels in vascular smooth muscle. Also inhibits sarco/endoplasmic reticulum Ca2+-ATPase (IC50 = 5 - 50 μM).
Technical Data
  • M.Wt:
    435.56
  • Formula:
    C27H33NO4
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Desiccate at -20°C
  • CAS No:
    57186-25-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels.
    Knaus et al.
    Biochemistry, 1994;33:5819
  2. Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel.
    Sanchez and McManus
    Neuropharmacology, 1996;35:963
  3. The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline.
    Bilmen et al.
    Arch.Biochem.Biophys., 2002;406:55

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