Bicuculline methochloride (Synonyms: (-)-Bicuculline methochloride)

Name: Bicuculline methochloride
Brand: MedChemExpress
SKU: HY-137790
Rating: 5.0 (39 reviews)

製品番号: HY-137790 純度: 99.80%: Data Sheet SDS COA 取扱説明書
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Bicuculline ((+)-Bicuculline; d-Bicuculline) methochloride is a selective GABAA receptor antagonist with an IC₅₀ value of 3 μM. Bicuculline methochloride induces clonic tonic convulsions in mammals and can also be used to block Ca²⁺ activated potassium channels. Bicuculline methochloride can be used in studies of epilepsy and other related psychiatric disorders.

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CAS 番号 : 38641-83-7

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 104	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 104	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$95	在庫あり	Estimated Time of Arrival: December 31
10 mg	$150	在庫あり	Estimated Time of Arrival: December 31
25 mg	$285	在庫あり	Estimated Time of Arrival: December 31
50 mg	$485	在庫あり	Estimated Time of Arrival: December 31
100 mg	$825	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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Based on 39 publication(s) in Google Scholar

Other Forms of Bicuculline methochloride:

Bicuculline methiodide 在庫あり
Bicuculline 在庫あり
Bicuculline methobromide お問い合わせ

顧客検証

In Vivo Efficacy Study

: Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 20:e07908. [Abstract]; GABAA receptor antagonist (Bicuculline, 5 µg/10 µL, i.t.) weakened acute morphine analgesic effect.

: Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Dec 16:e2407387. [Abstract]; Bicuculline (100 ng; 0.5 μL; infusion pump). Paw withdrawal responses to the 0.07 g von Frey filament following mPFC injection of physiological saline or Bicuculline (Bic) within 2 hours after intraperitoneal PTX injection.

: Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Cell. 2023 Mar 30;186(7):1352-1368.e18. [Abstract]; The antidepressant-like effect of activation of MGA1 in the FST was attenuated by A1 infusion of Bicuculline (BIC, 20 μM; infusion pump).

: Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Mar 28;12(7):3057-3078.; Bicuculline (3.5 mg/kg; subcutaneous injections). Western blot analyses of Gabra1, Gabra3, Gabra5, Gabrb3, Gabrg2, KCC2 and GAPDH in the lesion sites from different groups at 4 wpt.

: Bicuculline methochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Mar 28;12(7):3057-3078.; Bicuculline (3.5 mg/kg; subcutaneous injections). Representative IF images of transverse spinal cord sections from the Intact, +PBS, +PBS+Bic, +MSC, and +MSC+Bic groups at 4 wpt.

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製品説明

IC₅₀ & Target

IC50: 3 μM (GABA_A)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	7 3 Compound: 7	Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique	[PMID: 18998663]
HEK293	IC₅₀	7 3 Compound: 7	Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique	[PMID: 18998663]
HEK293	IC₅₀	7 3 Compound: 7	Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique	[PMID: 18998663]

体外実験

Bicuculline methochloride (1 μM and 3 μM) attains the maximal response of GABA. Bicuculline methochloride appears to shift the dose-response curves of GABA in parallel to the right without decreasing GABA maximal response, suggesting that it is a competitive antagonist at human α₁β₂γ_2L GABA_A receptors expressed in Xenopus oocytes^[3].
Bicuculline methochloride (1-100 μM; 2 min; applied as outside-out patches) potently blocks both Apamin (HY-P0256)-sensitive small-conductance calcium-activated potassium channels (SK2) currents and Apamin-insensitive SK1 currents in Xenopus oocytes^[4].

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

体内実験

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Bicuculline methochloride can be used in animal modeling to create epilepsy models. Intracerebral injection of Bicuculline methochloride causes an increase in capillary blood flow in the epileptic focus (the specific region where seizures originate), with local blood flow increasing to 42.5 red blood cells per second (compared to 27.8 red blood cells per second in areas away from the epileptic focus)^[5].

Induction of epilepsy^[5]

Background

Epileptic seizures are closely related to the imbalance between neuronal excitability and inhibition, leading to abnormal neuronal discharges. Bicuculline methochloride is a GABA_A receptor (GABAA receptor) antagonist that can inhibit inhibitory neurotransmission, induce excitatory neuronal activity, and cause population bursts (indicating that a large number of neurons fire action potentials simultaneously), thereby inducing epileptic seizures^[5].

Specific Modeling Methods

Mice: C57BL6 • male and female • 20-30 g
Administration: 2.5 mM • Intracranial Injection (deep layers of the somatosensory cortex) • single dose

Note

(1) Dissolve 2.5 mM bicuculline methochloride in physiological saline.
(2) Inject bicuculline methochloride by inserting a glass micropipette with a diameter of 20-50 μm into the deep layers of the mouse somatosensory cortex.
(3) Surgical operation precautions:
a. Fix an insulated metallic head frame above the planned craniotomy area, and make a craniotomy with a diameter of approximately 3 mm over the mouse somatosensory cortex, removing the dura mater to expose the brain tissue.
b. Gently rinse the exposed area with artificial cerebrospinal fluid (composition of artificial cerebrospinal fluid: 125 mM NaCl, 3 mM KCl, 26 mM NaHCO₃, 10 mM glucose, 1.1 mM NaH₂PO₄, 2 mM CaCl₂, 1 mM MgSO₄) to maintain the physiological environment of the brain tissue.
c. Cover the craniotomy with a phosphate-buffered saline solution containing 1% agarose (pH 7.4) and place a glass coverslip on the metal frame to protect the exposed brain tissue.

Modeling Indicators

Electrophysiological changes: A large number of neurons in the deep layers of the mouse somatosensory cortex fire electrical signals simultaneously, producing electrical signals characterized by interictal spikes (Note: Interictal Spikes (IISs) refer to the brief, high-amplitude voltage deflections observed in the electroencephalogram (EEG), which are typically associated with epileptic seizures).
Blood flow changes: In the somatosensory cortex of mice injected with bicuculline methochloride, capillary blood flow significantly increases.

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

分子量

417.84

分子式

C₂₁H₂₀ClNO₆

CAS 番号

38641-83-7

Appearance

Solid

Color

Light yellow to green yellow

SMILES

C[N+]([C@](C1=C2C=C3C(OCO3)=C1)([H])[C@@](O4)([H])C(C=CC5=C6OCO5)=C6C4=O)(CC2)C.[Cl-]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

H₂O : 50 mg/mL (119.66 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3933 mL	11.9663 mL	23.9326 mL
5 mM	0.4787 mL	2.3933 mL	4.7865 mL
10 mM	0.2393 mL	1.1966 mL	2.3933 mL

View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

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濃度 _（終了）

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.80%

Select Batch:

データシート (292 KB) SDS (252 KB)

COA (264 KB) HNMR (143 KB) RP-HPLC (163 KB) LCMS (232 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Y Yajima, et al. Effects of differential modulation of mu-, delta- and kappa-opioid systems on bicuculline-induced convulsions in the mouse. Brain Res. 2000 Apr 17;862(1-2):120-6. [Content Brief]

[2]. W A Turski, et al. Excitatory amino acid antagonists protect mice against seizures induced by bicuculline. Brain Res. 1990 Apr 23;514(1):131-4. [Content Brief]

[3]. Huang SH, et al. Bilobalide, a sesquiterpene trilactone from Ginkgo biloba, is an antagonist at recombinant alpha1beta2gamma2L GABA(A) receptors. Eur J Pharmacol. 2003;464(1):1-8. [Content Brief]

[4]. Khawaled R, et al. Bicuculline block of small-conductance calcium-activated potassium channels. Pflugers Arch. 1999 Aug;438(3):314-21. [Content Brief]

[5]. Hirase H, et al. Capillary level imaging of local cerebral blood flow in bicuculline-induced epileptic foci. Neuroscience. 2004;128(1):209-16. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	2.3933 mL	11.9663 mL	23.9326 mL	59.8315 mL
	5 mM	0.4787 mL	2.3933 mL	4.7865 mL	11.9663 mL
	10 mM	0.2393 mL	1.1966 mL	2.3933 mL	5.9832 mL
	15 mM	0.1596 mL	0.7978 mL	1.5955 mL	3.9888 mL
	20 mM	0.1197 mL	0.5983 mL	1.1966 mL	2.9916 mL
	25 mM	0.0957 mL	0.4787 mL	0.9573 mL	2.3933 mL
	30 mM	0.0798 mL	0.3989 mL	0.7978 mL	1.9944 mL
	40 mM	0.0598 mL	0.2992 mL	0.5983 mL	1.4958 mL
	50 mM	0.0479 mL	0.2393 mL	0.4787 mL	1.1966 mL
	60 mM	0.0399 mL	0.1994 mL	0.3989 mL	0.9972 mL
	80 mM	0.0299 mL	0.1496 mL	0.2992 mL	0.7479 mL
	100 mM	0.0239 mL	0.1197 mL	0.2393 mL	0.5983 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Bicuculline methochloride Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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.

Keywords:

Bicuculline methochloride38641-83-7(-)-Bicuculline methochlorideGABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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Bicuculline methochloride (Synonyms: (-)-Bicuculline methochloride)

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Other Forms of Bicuculline methochloride:

Bicuculline methochloride 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

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生物活性

純度とドキュメンテーション

参考文献

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Bicuculline methochloride 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Bicuculline methochloride Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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