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Home / Biochemicals / Small Molecules

(+)-Bicuculline

SKU : BHB21300053

A Potent Antagonist of GABA(A) Receptors

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Mfr.No.	B-135, B-135_100 mg, B-135_250 mg, B-135_50 mg, B-135_500 mg
Description	(+)-Bicuculline (#B-135) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C20H17NO6.
Background	gamma-Aminobutyric acid (GABA) is an amino acid derivate, synthesized from glutamate by the pyridoxal-L-phosphate (PLP)-dependent enzyme, glutamate decarboxylase (GAD)1. GABA provides the primary inhibitory signaling in the adult mammalian brain (CNS), and, to some degree of controversy, exerts a depolarizing response in the developing brain2.GABA is an agonist of two main receptor classes in the CNS: GABAA, an ionic ligand-gated channel, and GABAB, a metabotrophic, G-protein coupled receptor. GABAA is assembled by 5 out of 16 possible subunits with alpha, beta and either a gamma or a delta (2:2:1 stoichiometry) being the most common. With an EC50 between 3 to 12 uM it interacts with GABA to allow either an influx or an efflux of Cl- ions into and out of the cell, respectively3.Bicuculline (BIC) is a competitive allosteric inhibitor of GABAA-induced currents with an IC50 of 1-3 uM4. BIC has been employed to model epileptic seizures in hippocampal slices5, to induce schizophrenia-like symptoms in the pre-frontal cortex6, and is an essential research tool in the study of various psychomotor and behavioral defects4-6.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	1-100 uM.
Reconstitution	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. Repeat freeze-thawing may result in loss of activity
Cas Number	485-49-4
Molecular Weight	367.4
Solubility	DMSO (with gentle warming), DMF, chloroform. Centrifuge all product preparations before use (10000 x g 5 min).
Target	GABA(A) receptors
Source	Synthetic
Activity	(+)-Bicuculline inhibits (IC50 = 9 uM) recombinant alpha1beta1gamma2 GABA(A) channels that were activated with 3 uM GABA1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Cited Application: Electrophysiology Chemical Name: (R-(R,S))-6-(5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo(4,5-g)isoquinolin-5-yl)furo(3,4-e)-1,3-benzodioxol-8(6H)-one.

Purity	>99% (HPLC)
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. Storage of solutions: Up to four weeks at 4°C or three months at -20°C.

Product Manual	SDS

Reference	Briggs, S.W. and Galanopoulou, A.S. (2011) Neural Plast. 2011, 527605. Khakhalin, A.S. (2011) J. Neurophysiol. 106, 1065. Esmaeili, A. et al. (2009) J. Neurophysiol. 101, 341. Ueno, S. et al. (1997) J. Neurosci. 17, 625. Walker, J. et al. (2012) PLoS One 7, e31415. Paine, T.A. et al. (2011) Neuropsychopharmacology 36, 1703. Horne, A.L. et al. (1992) Br. J. Pharmacol. 107, 732.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300053-1	B-135_100 mg	100 mg	$92		Add to Cart
BHB21300053-2	B-135_250 mg	250 mg	$210		Add to Cart
BHB21300053-3	B-135_50 mg	50 mg	$76		Add to Cart
BHB21300053-4	B-135_500 mg	500 mg	$375		Add to Cart

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