Paxilline | Alomone Labs P-450 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

Paxilline

catalog :

P-450

more info or order :

Alomone Labs product webpage

citations: 21

Reference
Chang W, Wu S. Effective Activation of BKCa Channels by QO-40 (5-(Chloromethyl)-3-(Naphthalen-1-yl)-2-(Trifluoromethyl)Pyrazolo [1,5-a]pyrimidin-7(4H)-one), Known to Be an Opener of KCNQ2/Q3 Channels. Pharmaceuticals (Basel). 2021;14: pubmed publisher
Simkin D, Marshall K, Vanoye C, Desai R, Bustos B, Piyevsky B, et al. Dyshomeostatic modulation of Ca2+-activated K+ channels in a human neuronal model of KCNQ2 encephalopathy. elife. 2021;10: pubmed publisher
Chang W, Liu P, Wu S. Actions of FTY720 (Fingolimod), a Sphingosine-1-Phosphate Receptor Modulator, on Delayed-Rectifier K+ Current and Intermediate-Conductance Ca2+-Activated K+ Channel in Jurkat T-Lymphocytes. Molecules. 2020;25: pubmed publisher
Zhao H, Xue Q, Li C, Wang Q, Han S, Zhou Y, et al. Upregulation of Beta4 subunit of BKCa channels in the anterior cingulate cortex contributes to mechanical allodynia associated anxiety-like behaviors. Mol Brain. 2020;13:22 pubmed publisher
Huang M, Liu P, Wu S. Characterization of Perturbing Actions by Verteporfin, a Benzoporphyrin Photosensitizer, on Membrane Ionic Currents. Front Chem. 2019;7:566 pubmed publisher
Saeki T, Suzuki Y, Yamamura H, Takeshima H, Imaizumi Y. A junctophilin-caveolin interaction enables efficient coupling between ryanodine receptors and BKCa channels in the Ca2+ microdomain of vascular smooth muscle. J Biol Chem. 2019;294:13093-13105 pubmed publisher
Bondarenko A, Panasiuk O, Drachuk K, Montecucco F, Brandt K, Mach F. The quest for endothelial atypical cannabinoid receptor: BKCa channels act as cellular sensors for cannabinoids in in vitro and in situ endothelial cells. Vascul Pharmacol. 2018;102:44-55 pubmed publisher
Whitt J, McNally B, Meredith A. Differential contribution of Ca2+ sources to day and night BK current activation in the circadian clock. J Gen Physiol. 2018;150:259-275 pubmed publisher
Wu S, Chen H, Chou Y, Huang Y, Lo Y. Inhibitory actions by ibandronate sodium, a nitrogen-containing bisphosphonate, on calcium-activated potassium channels in Madin-Darby canine kidney cells. Toxicol Rep. 2015;2:1182-1193 pubmed publisher
Bondarenko A, Montecucco F, Panasiuk O, Sagach V, Sidoryak N, Brandt K, et al. GPR55 agonist lysophosphatidylinositol and lysophosphatidylcholine inhibit endothelial cell hyperpolarization via GPR-independent suppression of Na+-Ca2+ exchanger and endoplasmic reticulum Ca2+ refilling. Vascul Pharmacol. 2017;89:39-48 pubmed publisher
Nishijima Y, Cao S, Chabowski D, Korishettar A, Ge A, Zheng X, et al. Contribution of KV1.5 Channel to Hydrogen Peroxide-Induced Human Arteriolar Dilation and Its Modulation by Coronary Artery Disease. Circ Res. 2017;120:658-669 pubmed publisher
Iordache F, Constantinescu A, Andrei E, Amuzescu B, Halitzchi F, Savu L, et al. Electrophysiology, immunophenotype, and gene expression characterization of senescent and cryopreserved human amniotic fluid stem cells. J Physiol Sci. 2016;66:463-476 pubmed
VelÃ¡squez MartÃnez M, VÃ¡zquez Torres R, Rojas L, SANABRIA P, JimÃ©nez Rivera C. Alpha-1 adrenoreceptors modulate GABA release onto ventral tegmental area dopamine neurons. Neuropharmacology. 2015;88:110-21 pubmed publisher
Zhang Y, Yue J, Che H, Sun H, Tse H, Li G. BKCa and hEag1 channels regulate cell proliferation and differentiation in human bone marrow-derived mesenchymal stem cells. J Cell Physiol. 2014;229:202-12 pubmed publisher
Chen M, Sun H, Hu P, Wang C, Li B, Li S, et al. Activation of BKca channels mediates hippocampal neuronal death after reoxygenation and reperfusion. Mol Neurobiol. 2013;48:794-807 pubmed publisher
PEREZ G, Desai M, Anderson S, Scornik F. Large-conductance calcium-activated potassium current modulates excitability in isolated canine intracardiac neurons. Am J Physiol Cell Physiol. 2013;304:C280-6 pubmed publisher
Keating N, Quinlan L. Small conductance potassium channels drive ATP-activated chloride secretion in the oviduct. Am J Physiol Cell Physiol. 2012;302:C100-9 pubmed publisher
Ishii H, Nakajo K, Yanagawa Y, Kubo Y. Identification and characterization of Cs(+) -permeable K(+) channel current in mouse cerebellar Purkinje cells in lobules 9 and 10 evoked by molecular layer stimulation. Eur J Neurosci. 2010;32:736-48 pubmed publisher
Henney N, Li B, Elford C, Reviriego P, Campbell A, Wann K, et al. A large-conductance (BK) potassium channel subtype affects both growth and mineralization of human osteoblasts. Am J Physiol Cell Physiol. 2009;297:C1397-408 pubmed publisher
Griguoli M, Scuri R, Ragozzino D, Cherubini E. Activation of nicotinic acetylcholine receptors enhances a slow calcium-dependent potassium conductance and reduces the firing of stratum oriens interneurons. Eur J Neurosci. 2009;30:1011-22 pubmed publisher
Liu Y, Wang Y, Wu P, Wu S. Tramadol-induced block of hyperpolarization-activated cation current in rat pituitary lactotrophs. Naunyn Schmiedebergs Arch Pharmacol. 2009;379:127-35 pubmed publisher

image

image 1 :

Alomone Labs Paxilline inhibits KCa1.1 (BK) channels heterologously expressed in Xenopus oocytes. - Left: The effect of 100 nMPaxilline(#P-450) (a)Penitrem A(P-650) (b) andVerruculogen(#V-500) (c) on BK currents. Time course of current amplitude changes upon sequential application of the three toxins. Right: Example of current responses to 100 ms depolarization before (red) and during (black) perfusion of 500 nM Paxilline.

image 2 :

product information

CAT :

P-450

SKU :

P-450_0.45 mg

Product Name :

Paxilline

Group Type :

Non Antibodies

Product Type :

S. Molecules

Storage After Reconstitution :

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Shipping and storage :

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

Product Page - Scientific background :

Paxilline is a selective blocker of KCa1.1 (high-conductance Ca2+-activated K+, BK) channels. It belongs to a set of tremorgenic indole alkaloids which are lipid soluble and also include Penitrem A and Verruculogen.2Paxilline enhanced the electrically induced twitch contractions in guinea pig ileum, without influencing the contractions provoked by exogenous acetylcholine.1 Paxilline was shown to inhibit the peptidyle toxin resistant combination a+b4 channels (for more background see 3) expressed in CHO cells.4 It was shown to be as potent as Iberiotoxin in action potential broadening in hippocampus and amygdala.4,5Paxilline also inhibits intracellular Ca2+-ATPases (SERCA) with IC50s between 5 and 10 µM6.

Supplier :

Alomone Labs

Target :

KCa K+ channels, SERCA pump

Long Description :

Paxilline (#P-450) is a highly pure, natural, and biologically active compound.

Short Description :

A Mycotoxin Blocker of KCa1.1 (BK) Channels and SERCA Pumps

MW :

435.6

Source :

Natural

Molecular formula :

C27H33NO4.

Effective Concentration :

10-100 nM.

Activity :

Paxilline is a selective blocker of high-conductance Ca2+-activated (Maxi-K) K+ channels.

Reconstitution and Solubility :

Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity

Solubility :

DMSO or acetone. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions :

Up to one week at 4°C or three months at -20°C.

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Applications key :

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Purity :

>98% (HPLC)

CAS No :

57186-25-1

Form :

Lyophilized powder.

Comment :

Contact Alomone Labs for technical support and product customization

UNSPSC :

41116134

Bioassay Tested :

Yes

Chemical Name :

(2R,4bS,6aS,12bS,12cR,14aS)-5,6,6a,7,12,12b,12c,13,14,1 4a-Decahydro-4b-hydroxy-2-(1-hydroxy-1-methylethyl)-12b ,12c-dimethyl-2H-pyrano[2'',3'':5',6']benz[1',2':6,7]in deno[1,2-b]indol-3(4bH)-one.

more info or order :

Alomone Labs product webpage