Paxilline

Paxilline is an indole alkaloid mycotoxin derived from Penicillium paxilli, which effectively inhibits the BK channel through a channel-blocking mechanism. Paxilline also inhibits sarco/endoplasmic reticulum Ca2+-stimulated ATPase (SERCA), with IC50 values ranging from 5 μM to 50 μM for different SERCA isoforms. Paxilline exhibits significant anticonvulsant and neuroprotective effects, as well as certain antioxidant activity[1][2][3][4][5][6].

Product Specifications

CAS Number

[57186-25-1]

UNSPSC

12352005

Hazard Statement

H301, H311, H315, H318, H331, H335

Target

Calcium Channel; Potassium Channel; Reactive Oxygen Species (ROS)

Type

Natural Products

Related Pathways

Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/paxilline.html

Purity

99.91

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1[C@@H](C(C)(O)C)O[C@](CC2)([H])C([C@]([C@@]2(C)[C@]34C)(O)CC[C@@]3([H])CC5=C4NC6=C5C=CC=C6)=C1

Molecular Formula

C27H33NO4

Molecular Weight

435.56

Precautions

H301, H311, H315, H318, H331, H335

References & Citations

[1]Zhou Y, et al. Paxilline inhibits BK channels by an almost exclusively closed-channel block mechanism. J Gen Physiol. 2014 Nov;144 (5) :415-40.|[2]Bilmen JG, et al. The mechanism of inhibition of the sarco/endoplasmic reticulum Ca2+ ATPase by paxilline. Arch Biochem Biophys. 2002 Oct 1;406 (1) :55-64.|[3]Sheehan JJ, et al. Anticonvulsant effects of the BK-channel antagonist paxilline. Epilepsia. 2009 Apr;50 (4) :711-20.|[4]Kulawiak B, et al. Glutamate-induced cell death in HT22 mouse hippocampal cells is attenuated by paxilline, a BK channel inhibitor. Mitochondrion. 2012 Jan;12 (1) :169-72.|[5]Belyaeva EA, et al. Mitigating effect of paxilline against injury produced by Cd2+ in rat pheochromocytoma PC12 and ascites hepatoma AS-30D cells. Ecotoxicol Environ Saf. 2020 Jun 15;196:110519.|[6]Choi TY, et al. BK channel blocker paxilline attenuates thalidomide-caused synaptic and cognitive dysfunctions in mice. Sci Rep. 2018 Dec 5;8 (1) :17653.