Paxilline

Name: Paxilline
Brand: Tocris Bioscience
SKU: 2006
Rating: 5 (1 reviews)

Catalog # 2006 | Tocris Bioscience a Bio-Techne Brand

(1)

Citations (19)

COA / SDS

SERCA ATPase blocker. Also potent BKCa channel blocker

Key Product Details

Description:	SERCA ATPase blocker. Also potent BK_Ca 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)
Molecular Weight:	435.56

View Full Technical Details for Paxilline

Technical Data
Citations (19) / Reviews (1)

Biological Activity for Paxilline

Paxilline is a potent blocker of high-conductance Ca²⁺-activated K⁺ (BK_Ca, K_Ca1.1) channels. Binds to the α-subunit of BK_Ca (K_i = 1.9 nM for block of currents in α-subunit-expressing oocytes) and enhances binding of charybdotoxin to BK_Ca 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 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.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.30 mL	11.48 mL	22.96 mL
5 mM	0.46 mL	2.30 mL	4.59 mL
10 mM	0.23 mL	1.15 mL	2.30 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

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References for Paxilline

References are publications that support the biological activity of the product.

Bilmen The mechanism of inhibition of the sarco/endoplasmic reticulum Ca²⁺ ATPase by paxilline. Arch.Biochem.Biophys. 2002 PMID: 12234490
Sanchez and McManus Paxilline inhibition of the alpha-subunit of the high-conductance calcium-activated potassium channel. Neuropharmacology 1996 PMID: 8938726
Knaus Tremorgenic indole alkaloids potently inhibit smooth muscle high-conductance calcium-activated potassium channels. Biochemistry 1994 PMID: 7514038

Citations for Paxilline (19)

Showing 1 - 10 of 19 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for Paxilline include:

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
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
Abrahao et al. (2017) Ethanol-Sensitive Pacemaker Neurons in the Mouse External Globus Pallidus. Neuropsychopharmacology. 42:1070
PMID: 27827370
Whitt et al. (2016) BK channel inactivation gates daytime excitability in the circadian clock. Nat Commun. 7:10837
PMID: 26940770
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
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
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
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
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
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
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
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
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
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
Pyott et al. (2004) Extrasynaptic localization of inactivating calcium-activated potassium channels in mouse inner hair cells. FASEB J. 24:9469
PMID: 15509733

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Paxilline as a selective potassium blocker worked ideally to block SK channels

Name: Farzana Islam

Species: Human

Assay Type: In Vitro

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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