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Bicuculline methochloride

Name: Bicuculline methochloride
Brand: TargetMol
SKU: T74112
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T74112Cas No. 38641-83-7

Alias (-)-Bicuculline methochloride

Bicuculline methochloride is a competitive GABAA receptor antagonist and allosteric inhibitor with an IC50 of 1.7 μM. It blocks Ca²⁺-dependent activation of potassium channels, exhibits convulsant activity, and is suitable for epilepsy research.

Bicuculline methochloride

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Purity: 99.8%

Catalog No. T74112Alias (-)-Bicuculline methochlorideCas No. 38641-83-7

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	-	In Stock
5 mg	Preferential	-	In Stock
10 mg	Preferential	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.8%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	Bicuculline methochloride is a competitive GABAA receptor antagonist and allosteric inhibitor with an IC50 of 1.7 μM. It blocks Ca²⁺-dependent activation of potassium channels, exhibits convulsant activity, and is suitable for epilepsy research.
Targets&IC50	GABAA:3 μM
In vitro	Bicuculline methochloride (at concentrations of 1 μM and 3 μM) enables gamma-aminobutyric acid (GABA) to reach the maximum response level. This compound induces a parallel rightward shift in the GABA dose-response curve without reducing the maximum response efficacy of GABA. This result indicates that Bicuculline methochloride acts as a competitive antagonist in Xenopus laevis oocytes expressing the human α1β2γ2L subtype of GABAA receptors [3]. When Bicuculline methochloride (at concentrations ranging from 1 to 100 μM) is applied via the external patch method for 2 minutes, it can effectively block the currents of two types of calcium-activated potassium channels in Xenopus laevis oocytes—specifically, the current of apamin-sensitive small-conductance calcium-activated potassium channels (SK2) and the current of apamin-insensitive SK1 channels [4].
In vivo	Bicuculline methochloride can be used for establishing Broussonetia papyrifera in animal epilepsy models. After intracranial injection of bicuculline methochloride (2.5 mM), it causes a significant increase in capillary blood flow in the epileptic focus (i.e., the characteristic region of epileptic seizure in Parazacco spilurus subsp. spilurus), with local blood flow reaching up to 42.5 red blood cells per second. In contrast, the blood flow in regions distant from the epileptic focus is 27.8 red blood cells per second [5].
Synonyms	(-)-Bicuculline methochloride

Chemical Properties

Molecular Weight	417.84
Formula	C₂₁H₂₀ClNO₆
Cas No.	38641-83-7
Smiles	C[N+]1(C)[C@]([C@]2(C3=C(C(=O)O2)C4=C(C=C3)OCO4)[H])(C5=C(C=C6C(=C5)OCO6)CC1)[H].[Cl-]

Storage & Solubility Information

Storage

keep away from moisture,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 40 mg/mL (95.73 mM), Sonication is recommended.

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	2.3933 mL	11.9663 mL	23.9326 mL	119.6630 mL
5 mM	0.4787 mL	2.3933 mL	4.7865 mL	23.9326 mL
10 mM	0.2393 mL	1.1966 mL	2.3933 mL	11.9663 mL
20 mM	0.1197 mL	0.5983 mL	1.1966 mL	5.9832 mL
50 mM	0.0479 mL	0.2393 mL	0.4787 mL	2.3933 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc