Name: Paxilline
Brand: Alomone Labs
SKU: P-450

Overview

Cat #: P-450

Lyophilized Powder yes

Origin Penicillium paxilli.

Source Natural

MW: 435.6

Purity: >98% (HPLC)

Effective concentration 10-100 nM.

Structure

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.

Molecular formula C₂₇H₃₃NO₄.

CAS No.: 57186-25-1

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

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.

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.

Our bioassay

Alomone Labs Paxilline inhibits K_Ca1.1 (BK) channels heterologously expressed in Xenopus oocytes.
Left: The effect of 100 nM Paxilline (#P-450) (a), Penitrem A (P-650) (b), and Verruculogen (#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.

References - Scientific background

Selala, M.I. et al. (1991) J. Nat. Prod. 54, 207.
Knaus, H.G. et al. (1994) Biochemistry 33, 5819.
Modulator Issue No. 17.pdf
Hu, H. et al. (2001) J. Neurosci. 21, 9585.
Faber, E.S. and Sah, P. (2002) J. Neurosci. 22, 1618.
Bilmen, J.G. et al. (2002) Arch. Biochem. Biophys. 406, 55.

Scientific background

Paxilline is a selective blocker of K_Ca1.1 (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.²

Paxilline 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.^4,5

Paxilline also inhibits intracellular Ca²⁺-ATPases (SERCA) with IC₅₀s between 5 and 10 µM⁶.

Target K_Ca K⁺ channels, SERCA pump

Lyophilized Powder

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

Certificate of Analysis SDS

Image & Title

Alomone Labs Paxilline inhibits K_Ca1.1 channel currents in isolated canine intracardiac neurons.Representative current traces show a total blockage of the fast-activated current component and a reduction of the slow outward component caused by 100 nM Paxilline (#P-450).Adapted from Perez, G.J. et al. (2013) Am. J. Physiol. 304, C280. with permission of The American Physiological Society.

For research purposes only, not for human use

Last Update: 07/05/2024

Applications

Citations

Product citations

Iordache, F. et al. (2016) J. Physiol. Sci. 66, 463.
Zhang, Y.Y. et al. (2014) J. Cell. Phys. 229, 202.
Chen, M. et al. (2013) Mol. Neurobiol. 48, 794.
Perez, G.J. et al. (2013) Am. J. Physiol. 304, C280.
Keating, N. and Quinlan, L.R. (2012) Am. J. Physiol. 302, C100.
Ishii, H. et al. (2010) Eur. J. Neurosci. 32, 736.
Henney, N.C. et al. (2009) Am. J. Physiol. 297, C1397.
Griguoli, M. et al. (2009) Eur. J. Neurosci. 30, 1011.
Benhassine, N. and Berger, T. (2009) Pflugers Arch. 457, 1133.
Liu, Y.C. et al. (2009) Naunyn-Schmiedeberg's Arch. Pharmacol. 379, 127.
Wu, S.N. et al. (2008) Mol. Pharmacol. 74, 1696.

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Paxilline

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Scientific Background

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