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Bicuculline

Name: Bicuculline
Brand: TargetMol
SKU: T2850
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: d-Bicuculline, (+)-Bicuculline) Copy Product Info

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Synonyms: d-Bicuculline, (+)-Bicuculline

Catalog No. T2850 Copy Product Info

Purity: 99.99%

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Bicuculline is an alkaloid extracted from Corydalis decumbens, acting as a competitive antagonist of the neurotransmitter GABAA receptor (IC50 = 2 μM). Bicuculline also blocks Ca2+-activated potassium (SK) channels and inhibits slow afterhyperpolarization (slow AHP). Bicuculline has anticonvulsant effects and is commonly used to establish mouse seizure models.

Cas No. 485-49-4

Pack Size	Price	USA Stock	Global Stock
10 mg	$30	In Stock	In Stock
25 mg	$43	In Stock	In Stock
50 mg	$63	In Stock	In Stock
100 mg	$90	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.99%

Color:White to Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Bicuculline is an alkaloid extracted from Corydalis decumbens, acting as a competitive antagonist of the neurotransmitter GABAA receptor (IC50 = 2 μM). Bicuculline also blocks Ca2+-activated potassium (SK) channels and inhibits slow afterhyperpolarization (slow AHP). Bicuculline has anticonvulsant effects and is commonly used to establish mouse seizure models.
Targets & IC50	GABAA receptor:2 μM
In vitro	Methods: In hippocampal CA1 pyramidal neurons from WT and PGC-1α−/− mice, Bicuculline (1 μM) was applied via bath-dialysis. Following stable perfusion, the I/E ratio was calculated from whole-cell voltage-clamp recordings. Results: PGC-1α−/− mice exhibited approximately double the amplitude of double-synaptic IPSCs compared to WT mice, with a significantly elevated I/E ratio. Bicuculline restored both IPSCs and the I/E ratio in PGC-1α−/− mice to WT levels without affecting EPSCs. [1] Methods: Bicuculline (100 μM) and GABA (50 μM) were added to neonatal mouse (P5) cerebellar cultured astrocytes. GABA was applied for 30 s at 7-minute intervals, and whole-cell patch-clamp recordings were performed. Results: Bicuculline (100 μM) blocked (90.5 ± 3.7%) the currents induced by 50 μM GABA. [2]
In vivo	Methods: Male SD rats received subcutaneous injections of Bicuculline (1, 4 mg/kg). Blood and brain tissue samples were collected at 10, 30, and 110 min post-administration. Plasma and brain tissue drug concentrations were measured by LC-MS/MS. Seizure grades were observed and recorded. Results: Bicuculline exhibited dose-dependent brain penetration. Tmax in brain tissue was 10 min in the 1 mg/kg group and 30 min in the 4 mg/kg group. Seizures (≥ Grade III) were induced at brain concentrations >880 ng/g.[2]
Synonyms	d-Bicuculline, (+)-Bicuculline

Chemical Properties

Molecular Weight	367.35
Formula	C₂₀H₁₇NO₆
Cas No.	485-49-4
Smiles	[H][C@]1(OC(=O)c2c3OCOc3ccc12)[C@@]1([H])N(C)CCc2cc3OCOc3cc12
Relative Density.	1.3694 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 16.67 mg/mL (45.38 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.44 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7222 mL	13.6110 mL	27.2220 mL	136.1100 mL
5 mM	0.5444 mL	2.7222 mL	5.4444 mL	27.2220 mL
10 mM	0.2722 mL	1.3611 mL	2.7222 mL	13.6110 mL
20 mM	0.1361 mL	0.6805 mL	1.3611 mL	6.8055 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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