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Submit ReviewPaxilline
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% (HPLC)
Biological Activity for Paxilline
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).
Compound Libraries for Paxilline
Paxilline is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Paxilline
| M. Wt | 435.56 |
| Formula | C27H33NO4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 57186-25-1 |
| PubChem ID | 105008 |
| InChI Key | ACNHBCIZLNNLRS-UBGQALKQSA-N |
| Smiles | [H][C@@]4([C@](C)3[C@]5(C)[C@@](C([C@]6([H])CC5)=CC([C@@H]([C@](O)(C)C)O6)=O)(O)CC4)CC2=C3NC1=CC=CC=C12 |
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.
Solubility Data for Paxilline
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.56 | 100 | |
| ethanol | 8.71 | 20 |
Preparing Stock Solutions for Paxilline
The following data is based on the product molecular weight 435.56. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for Paxilline
References for Paxilline
References are publications that support the biological activity of the product.
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, 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, Channels, 2006, Tocris Bioscience
19 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
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
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
Whitt et al (2016) BK channel inactivation gates daytime excitability in the circadian clock. Nat Commun 7 10837 PMID: 26940770
Madry et al (2018) Microglial Ramification, Surveillance, and Interleukin-1β Release Are Regulated by the Two-Pore Domain K+ Channel THIK-1. Neuron 97 299 PMID: 29290552
Abrahao et al (2017) Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus. Neuropsychopharmacology 42 1070 PMID: 27827370
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
Wan et al (2013) Reduced vascular smooth muscle BK channel current underlies heart failure-induced vasoconstriction in mice. Nat Commun 27 1859 PMID: 23325318
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
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
Zhang et al (2009) Tamoxifen mediated estrogen receptor activation protects against early impairment of hippocampal neuron excitability in an oxygen/glucose deprivation brain slice ischemia model. Brain Res 1247 196 PMID: 18992727
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
Westcott et al (2012) Function and expression of ryanodine receptors and inositol 1,4,5-trisphosphate receptors in smooth muscle cells of murine feed arteries and arterioles. J Physiol 590 1849 PMID: 22331418
Pulkkinen et al (2012) The bitter taste receptor (TAS2R) agonists denatonium and chloroquine display distinct patterns of relaxation of the guinea pig trachea. Am J Physiol Lung Cell Mol Physiol 303 L956 PMID: 22962016
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
Fernadez-Fernandez et al (2018) Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons. PLoS One 13 e0199282 PMID: 29928032
Pyott et al (2004) Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells. FASEB J 24 9469 PMID: 15509733
Zhang et al (2008) Resveratrol attenuates early pyramidal neuron excitability impairment and death in acute rat hippocampal slices caused by oxygen-glucose deprivation. Exp Neurol 212 44 PMID: 18495119
Do you know of a great paper that uses Paxilline from Tocris? Please let us know.
Reviews for Paxilline
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Paxilline as a selective potassium blocker worked ideally to block SK channels.
By
Farzana Islam on 10/06/2018
Assay Type: In Vitro
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.
