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
11 Citations for Paxilline
Citations are publications that use Tocris products. Selected citations for Paxilline include:
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
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
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
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
Parajuli et al (2014) 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. Eur J Pharmacol 738 179 PMID: 24886877
Ksiazek et al (2013) Properties of BK-type Ca(+) (+)-dependent K(+) channel currents in medial prefrontal cortex pyramidal neurons in rats of different ages. Front Cell Neurosci 7 185 PMID: 24312002
Bodhinathan et al (2010) Redox sensitive calcium stores underlie enhanced after hyperpolarization of aged neurons: role for ryanodine receptor mediated calcium signaling. J Neurophysiol 104 2586 PMID: 20884759
Pyott et al (2004) Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells. FASEB J 24 9469 PMID: 15509733
Simkin et al (2015) Aging-Related Hyperexcitability in CA3 Pyramidal Neurons Is Mediated by Enhanced A-Type K+ Channel Function and Expression. J Neurosci 35 13206 PMID: 26400949
Wan et al (2013) Reduced vascular smooth muscle BK channel current underlies heart failure-induced vasoconstriction in mice. Nat Commun 27 1859 PMID: 23325318
Do you know of a great paper that uses Paxilline from Tocris? If so please let us know.
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