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).
|Storage||Desiccate at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 435.56. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.3 mL||11.48 mL||22.96 mL|
|5 mM||0.46 mL||2.3 mL||4.59 mL|
|10 mM||0.23 mL||1.15 mL||2.3 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References are publications that support the products' biological activity.
Knaus et al (1994) Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 33 5819 PMID: 7514038
Sanchez and McManus (1996) Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology 35 963 PMID: 8938726
Bilmen et al (2002) The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline. Arch.Biochem.Biophys. 406 55 PMID: 12234490
If you know of a relevant reference for Paxilline, please let us know.
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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, Ca2+-Activated, Potassium, Channels, Ca2+-ATPase, Ca2+-ATPase, Tocris Bioscience
7 Citations for Paxilline
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.
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