Catalog # Availability Size / Price Qty
Paxilline | CAS No. 57186-25-1 | Ca2+-ATPase Blockers
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Description: SERCA ATPase blocker. Also potent BKCa channel blocker

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

Purity: ≥98%

Product Details
Citations (19)
Reviews (1)

Biological Activity

Paxilline is a 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

Soluble to 100 mM in DMSO and to 20 mM in ethanol
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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Citations for Paxilline

The citations listed below are publications that use Tocris products. Selected citations for Paxilline include:

19 Citations: Showing 1 - 10

  1. Microglial Ramification, Surveillance, and Interleukin-1β Release Are Regulated by the Two-Pore Domain K+ Channel THIK-1.
    Authors: Madry Et al.
    Neuron  2018;97:299
  2. Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons.
    Authors: Fernadez-Fernandez Et al.
    PLoS One  2018;13:e0199282
  3. Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus.
    Authors: Abrahao Et al.
    Neuropsychopharmacology  2017;42:1070
  4. BK channel inactivation gates daytime excitability in the circadian clock.
    Authors: Whitt Et al.
    Nat Commun  2016;7:10837
  5. Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction.
    Authors: Kim Et al.
    J Neurophysiol  2015;35:8245
  6. BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells.
    Authors: Hirono Et al.
    J Neurosci  2015;35:7082
  7. Aging-Related Hyperexcitability in CA3 Pyramidal Neurons Is Mediated by Enhanced A-Type K+ Channel Function and Expression.
    Authors: Simkin Et al.
    J Neurosci  2015;35:13206
  8. Prostaglandin E2 excitatory effects on guinea pig urinary bladder smooth muscle: a novel regulatory mechanism mediated by large-conductance voltage- and Ca2+-activated K+ channels.
    Authors: Parajuli Et al.
    Eur J Pharmacol  2014;738:179
  9. BK channels regulate sinoatrial node firing rate and cardiac pacing in vivo.
    Authors: Lai Et al.
    Am J Physiol Heart Circ Physiol  2014;307:H1327
  10. Properties of BK-type Ca(+) (+)-dependent K(+) channel currents in medial prefrontal cortex pyramidal neurons in rats of different ages.
    Authors: Ksiazek Et al.
    Front Cell Neurosci  2013;7:185
  11. Mis-expression of the BK K(+) channel disrupts suprachiasmatic nucleus circuit rhythmicity and alters clock-controlled behavior.
    Authors: Montgomery Et al.
    Am J Physiol Cell Physiol  2013;304:C299
  12. Reduced vascular smooth muscle BK channel current underlies heart failure-induced vasoconstriction in mice.
    Authors: Wan Et al.
    Nat Commun  2013;27:1859
  13. Function and expression of ryanodine receptors and inositol 1,4,5-trisphosphate receptors in smooth muscle cells of murine feed arteries and arterioles.
    Authors: Westcott Et al.
    J Physiol  2012;590:1849
  14. The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea.
    Authors: Pulkkinen Et al.
    Am J Physiol Lung Cell Mol Physiol  2012;303:L956
  15. Redox sensitive calcium stores underlie enhanced after hyperpolarization of aged neurons: role for ryanodine receptor mediated calcium signaling.
    Authors: Bodhinathan Et al.
    J Neurophysiol  2010;104:2586
  16. Mechanisms of sustained high firing rates in two classes of vestibular nucleus neurons: differential contributions of resurgent Na, Kv3, and BK currents.
    Authors: Gittis Et al.
    J Neurosci  2010;104:1625
  17. Tamoxifen mediated estrogen receptor activation protects against early impairment of hippocampal neuron excitability in an oxygen/glucose deprivation brain slice ischemia model.
    Authors: Zhang Et al.
    Brain Res  2009;1247:196
  18. Resveratrol attenuates early pyramidal neuron excitability impairment and death in acute rat hippocampal slices caused by oxygen-glucose deprivation.
    Authors: Zhang Et al.
    Exp Neurol  2008;212:44
  19. Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells.
    Authors: Pyott Et al.
    FASEB J  2004;24:9469


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Paxilline as a selective potassium blocker worked ideally to block SK channels
By Farzana Islam on 10/06/2018
Application: Species: Human

High-affinity and specific potassium channel blocker, used to study how it works to block SK (small conductance) channels. The product dissolved in DMSO and was excellent under lab conditions. Inhibition of SK channels were observed.

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