Art. -Nr.: HY-B1494

Picrotoxinin

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors. Picrotoxinin inhibits α₁β₂γ_2L GABA_A receptor with an IC₅₀ of 1.15 μM.

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Reinheit: 99.91%
CAS. Nr.: 17617-45-7
Formel: C₁₅H₁₆O₆
Molecular Weight:292.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Picrotoxinin Chemical Structure

CAS. Nr.: 17617-45-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1.15 μM (GABA_A receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	2.4 μM Compound: PXN, picrotoxinin	Inhibition of rat alpha2 homomeric glycine receptor expressed in CHO cells assessed as inhibition of 300 uM glycine-elicited current by outside patch clamp technique Inhibition of rat alpha2 homomeric glycine receptor expressed in CHO cells assessed as inhibition of 300 uM glycine-elicited current by outside patch clamp technique	[PMID: 17405877]

In Vitro

Picrotoxinin (0.001 μM-1 mM; 60-90 s) inhibits the action of GABA_A receptor and regulates GABA_A modulators in the presence of EC₅ GABA at α₁β₂γ_2L GABA_A receptors^[1].

MedChemExpress (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 GABA_A 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 α₁β₂γ_2L GABA_A receptors with IC₅₀s of 0.55, 0.49, 0.35-0.36, 0.50, 0.14 and 0.44 μM, respectively.

Chemical Information

CAS. Nr. 17617-45-7
Appearance Solid
Molecular Weight 292.28
Formel C₁₅H₁₆O₆
Color White to off-white
SMILES

O=C1[C@]([C@@H]2C(C)=C)([H])[C@]3(O)C[C@]4([H])[C@](O4)(C(O5)=O)[C@]3(C)[C@@]5([H])[C@]2([H])O1
Structure Classification
- Terpenoids
- Sesquiterpenes
Initial Source
- Plants
- other families
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Journal Impact Factor

Cell Death Discov

ALG13 participates in epileptogenesis via regulation of GABAA receptors in mouse models. [Abstract]

2020 Sep 17;6(1):87. PMID: 33014431
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
Neuropharmacology

Molecular mechanisms of action determine inhibition of paroxysmal depolarizing shifts by NMDA receptor antagonists in rat cortical neurons. [Abstract]

2021 Feb 15:184:108443. PMID: 33345828
J Neurochem

Somatostatin interneurons inhibit excitatory transmission mediated by astrocytic GABAB and presynaptic GABAB and adenosine A1 receptors in the hippocampus. [Abstract]

2022 Nov;163(4):310-326. PMID: 35775994

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (342.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ng CC, et al. Effects of bilobalide, ginkgolide B and picrotoxinin on GABA_A receptor modulation by structurally diverse positive modulators. Eur J Pharmacol. 2017 Jul 5;806:83-90. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4214 mL	17.1069 mL	34.2138 mL	85.5344 mL
	5 mM	0.6843 mL	3.4214 mL	6.8428 mL	17.1069 mL
	10 mM	0.3421 mL	1.7107 mL	3.4214 mL	8.5534 mL
	15 mM	0.2281 mL	1.1405 mL	2.2809 mL	5.7023 mL
	20 mM	0.1711 mL	0.8553 mL	1.7107 mL	4.2767 mL
	25 mM	0.1369 mL	0.6843 mL	1.3686 mL	3.4214 mL
	30 mM	0.1140 mL	0.5702 mL	1.1405 mL	2.8511 mL
	40 mM	0.0855 mL	0.4277 mL	0.8553 mL	2.1384 mL
	50 mM	0.0684 mL	0.3421 mL	0.6843 mL	1.7107 mL
	60 mM	0.0570 mL	0.2851 mL	0.5702 mL	1.4256 mL
	80 mM	0.0428 mL	0.2138 mL	0.4277 mL	1.0692 mL
	100 mM	0.0342 mL	0.1711 mL	0.3421 mL	0.8553 mL

Keywords

Picrotoxinin

4 Cited Publications

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Picrotoxinin

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Publications Citing Use of MedChemExpress (MCE) Picrotoxinin

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Picrotoxinin Related Classifications

HY-B1494 Related Classifications