Paxilline

Cat. No. 2006

Paxilline C27H33NO4 [57186-25-1]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Bilmen et al (2002) The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline. Arch.Biochem.Biophys. 406 55. PMID: 12234490.

Sanchez and McManus (1996) Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology 35 963. PMID: 8938726.

Knaus et al (1994) Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33 5819. PMID: 7514038.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Paxilline include:

Hirono et al (2015) BK Channels Localize to the Paranodal Junction and Regulate Action Potentials in Myelinated Axons of Cerebellar Purkinje Cells. J Neurosci 35 7082. PMID: 25948259.

Kim et al (2015) Astrocyte contributions to flow/pressure-evoked parenchymal arteriole vasoconstriction. J Neurophysiol 35 8245. PMID: 26019339.

Lai et al (2014) BK channels regulate sinoatrial node firing rate and cardiac pacing in vivo. Am J Physiol Heart Circ Physiol 307 H1327. PMID: 25172903.

Montgomery et al (2013) Mis-expression of the BK K(+) channel disrupts suprachiasmatic nucleus circuit rhythmicity and alters clock-controlled behavior. Am J Physiol Cell Physiol 304 C299. PMID: 23174562.

Wan et al (2013) Reduced vascular smooth muscle BK channel current underlies heart failure-induced vasoconstriction in mice. Nat Commun 27 1859. PMID: 23325318.

Gittis et al (2010) Mechanisms of sustained high firing rates in two classes of vestibular nucleus neurons: differential contributions of resurgent Na, Kv3, and BK currents. J Neurosci 104 1625. PMID: 20592126.

Pyott et al (2004) Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells. FASEB J 24 9469. PMID: 15509733.

Do you know of a great paper that uses Paxilline from Tocris? If so please let us know.show all ▼show less ▲

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Keywords: Paxilline, supplier, Potent, blockers, BKCa, channels, SERCA, ATPases, Potassium, ca2+-activated, ca2+-dependent, Ca2+-ATPase, Signaling, Signalling, Calcium, Calcium-ATPase, Ion, Transporters, Pumps, Tocris Bioscience, Ca2+-ATPase Blocker products

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