(+)-Bicuculline

Catalog No.S7071 Batch:S707107

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Technical Data

Formula

C20H17NO6
Molecular Weight 367.35 CAS No. 485-49-4
Solubility (25°C)* In vitro DMSO 73 mg/mL (198.72 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
1.21mg/ml Taking the 1 mL working solution as an example, add 50 μL of 24.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description (+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
Targets
GABAA receptor [1]
2 μM
In vitro (+)-Bicuculline (1-100μM) dose-dependently inhibits the Cl- conductance generated by 40 μM GABA. (+)-Bicuculline also inhibits the agonist action of GABA at 40 μM at α1β2γ2L receptors. (+)-Bicuculline at 1 and 3 μM increases GABA EC50 values 1.6 times (41.0-67.0 μM) and 3.6 times (36.1-129.0 μM), respectively. Atα1β2γ2L GABAA receptors, (+)-bicuculline displays the general property of the competitive antagonist, producing a parallel shift of GABA concentration-effect curves and having no effect on the maximal response of GABA. [1] In addition to being a potent GABAA receptor antagonist, (+)-bicuculine also blocks Ca2+-activated potassium channels. [2]

Protocol (from reference)

Customer Product Validation

, , Sci Rep, 2014, 4:7270.

Data from [Data independently produced by , , Br J Pharmacol, 2016, 173(10):1693-702.]

Data from [Data independently produced by , , Sci Rep, 2016, 6: 19266.]

Selleck's (+)-Bicuculline has been cited by 17 publications

Neuronal excitation-inhibition imbalance in the basolateral amygdala is involved in propofol-mediated enhancement of fear memory [ Commun Biol, 2024, 7(1):1408] PubMed: 39472670
Prenatal valproic acid on the basis of gestational diabetes also induces autistic behavior and disrupts myelination and oligodendroglial maturation slightly in offspring [ Research Square, 2024, 10.21203/rs.3.rs-3480364/v1] PubMed: none
Inhibition of GABAA receptors in intestinal stem cells prevents chemoradiotherapy-induced intestinal toxicity [ J Exp Med, 2022, 219-12e20220541] PubMed: 36125780
Antidepressant-like effects of cinnamamide derivative M2 via D2 receptors in the mouse medial prefrontal cortex [ Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7] PubMed: 35079131
Propofol alleviates PTSD-like behavioral deficits by downregulating hippocampal Arc associated with GABAergic activation in basolateral amygdala in rats [ Research Square, 2022, 10.21203/rs.3.rs-2349261/v1] PubMed: none
Neuritin improves the neurological functional recovery after experimental intracerebral hemorrhage in mice [ Neurobiol Dis, 2021, 156:105407] PubMed: 34058347
Terahertz exposure enhances neuronal synaptic transmission and oligodendrocyte differentiation in vitro [ iScience, 2021, 24(12):103485] PubMed: 34927027
Unraveling Autocrine Signaling Pathways through Metabolic Fingerprinting in Serous Ovarian Cancer Cells [ Biomedicines, 2021, 9(12)1927] PubMed: 34944743
N-Demethylsinomenine, an active metabolite of sinomenine, attenuates chronic neuropathic and inflammatory pain in mice [ Sci Rep, 2021, 11(1):9300] PubMed: 33927244
The Meningioma Enhancer Landscape Delineates Novel Subgroups and Drives Druggable Dependencies [ Cancer Discov, 2020, CD-20-0160] PubMed: 32703768

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.