1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. Chloride Channel
    GABA Receptor
  3. Picrotoxinin

Picrotoxinin 

Cat. No.: HY-B1494 Purity: ≥98.0%
COA Handling Instructions

Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.

For research use only. We do not sell to patients.

Picrotoxinin Chemical Structure

Picrotoxinin Chemical Structure

CAS No. : 17617-45-7

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10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

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Description

Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM[1].

IC50 & Target

IC50: 1.15 μM (GABAA receptor)[1]

In Vitro

Picrotoxinin (0.001 µM-1 mM; 60-90 s) inhibits the action of GABAA receptor and regulates GABAA modulators in the presence of EC5 GABA at α1β2γ2L GABAA receptors[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Xenopus oocytes
Concentration: 0.001 µM-1 mM
Incubation Time: 60 and 90 s
Result: Dose-dependently inhibited the action of GABAA receptor with an IC50 of 1.15 µM and exhibited the most potent activity compared with bilobalide and ginkgolide B. Inhibited etomidate, propofol, diazepam, thiopentone sodium, loreclezole and allopregnanoloner in the presence of EC5 GABA at α1β2γ2L GABAA receptors with IC50s of 0.55, 0.49, 0.35-0.36, 0.50, 0.14 and 0.44 μM, respectively.
Molecular Weight

292.28

Formula

C15H16O6

CAS No.
SMILES
Structure Classification
Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (342.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4214 mL 17.1069 mL 34.2138 mL
5 mM 0.6843 mL 3.4214 mL 6.8428 mL
10 mM 0.3421 mL 1.7107 mL 3.4214 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.55 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: ≥98.0%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Picrotoxinin
Cat. No.:
HY-B1494
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