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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 HNMR LCMS

Product Information

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
Disease Modeling Protocol	Focal Epilepsy Model Modeling Mechanism： Bicuculline, as a competitive antagonist of γ-aminobutyric acid A (GABAₐ) receptors, induces epilepsy pathology through multiple mechanisms: ① It blocks GABAₐ receptor-mediated inhibitory synaptic transmission, disrupting the excitability/inhibition balance in the brain, triggering local neuronal overexcitation, and forming focal epileptic seizures; ② It induces hemodynamic changes (increased optical absorption coefficient) in the epileptic focus area, accompanied by abnormal interictal discharges on electroencephalography (EEG), mimicking the core pathological and electrophysiological characteristics of human neocortical epilepsy. Modeling Method： Experimental Subject： Male Sprague-Dawley rats (250–500 g) Dosage and Administration Route： Dosage and route of administration:Neocortical focus: Epidural injection of bicuculline methiodide (BMI), 4 mM, 5 μl. Followed by a flush of 40 ul lactated Ringer’s solution into the epidural space. Hippocampal focus: Intrahippocampal injection of BMI, 0.1 mM, 2 μl. Dosing Frequency and Duration Model： Single dose Validation： Electrophysiological indicators: EEG recording: Typical epileptiform discharges (increased amplitude, abnormal frequency) appeared after modeling, lasting for more than 6 minutes, while no abnormal discharges were observed in the control group; Optical imaging: DOT detection showed a significant increase in the optical absorption coefficient of the epileptic focus area (P<0.05 vs. resting state), which could accurately locate epileptic foci with an injection depth of 1-3 mm. ESL was used for auxiliary verification, but there was a slight horizontal offset; Specificity verification: When BMI was injected outside the field of view of the DOT/ESL probe, DOT showed a negative detection (no epileptic focus signal), and ESL may show false positives, confirming the specificity of DOT localization; Behavioral indicators: After modeling, focal limb twitching, stereotyped movements, and other focal epileptic seizure manifestations appeared, without generalized tonic-clonic seizures (consistent with the characteristics of focal epilepsy). Precautions： 1. Methylene blue (MB, at a concentration of 1–2 mg in the perfusion solution) was added to the injection solution to allow for visual observation of the perfusion solution’s spread after the rats were euthanized.2. Due to drug leakage, some rats required 2–3 injections. Specifically, 14 rats received a single injection, 7 rats received two injections, and 2 rats received three injections. The total injection volume was 7.5 microliters. References：Eder HG, et al. Local perfusion of diazepam attenuates interictal and ictal events in the bicuculline model of epilepsy in rats. Epilepsia. 1997 May;38(5):516-21.

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

Keep away from direct sunlight, Pure form: -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

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Please see Product 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