CGP 7930

Name: CGP 7930
Brand: Tocris Bioscience
SKU: 1513

Tocris Bioscience, part of Bio-Techne | Catalog # 1513

Citations (21)

COA / SDS

Positive allosteric modulator of GABAB receptors

Key Product Details

Description:	Positive allosteric modulator of GABA_B receptors
Chemical Name:	3,5-bis(1,1-Dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol
Purity:	≥98% (HPLC)
Molecular Weight:	292.46

View Full Technical Details for CGP 7930

Technical Data
Citations

Biological Activity for CGP 7930

CGP 7930 is a positive allosteric modulator of GABA_A and GABA_B receptors. Increases the potency and efficacy of GABA at both recombinant and native GABA_B receptors (EC₅₀ values are 4.60 μM and 5.37 μM respectively) and enhances the inhibitory effect of the agonist L-baclofen in cultured cortical neurons. In HEK-293 cells expressing recombinant GABA_A receptor, CGP 7930 increases the potency and efficacy of GABA (EC₅₀ values are 1.0 μM and 1.7 μM at α4β3δ and α1β2γ2L receptors respectively). In cultured hippocampal neurons, pre-application of CGP 7930 causes concentration-dependent potentiation of GABA_A receptor currents by specific type-A receptor agonist Muscimol (EC₅₀ = 2.0 μM). CGP7930 potentiates GABA_A receptor-mediated tonic inhibition, reduces the frequency of inhibitory postsynaptic currents and prolongs rise and decay times. CGP 7930 also blocks G protein-coupled inwardly rectifying K+ (GIRK) channels diminishing GABA_A receptor signaling in HEK 293 cells. CGP 7930 reduces operant self-administration of ethanol in alcohol-preferring rats following i.p. administration.

Compound Libraries for CGP 7930

CGP 7930 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for CGP 7930

M. Wt	292.46
Formula	C₁₉H₃₂O₂
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	57717-80-3
PubChem ID	5024764
InChi Key	XLWJPQQFJNGUPA-UHFFFAOYSA-N
Smiles	CC(C)(CO)CC1=CC(=C(O)C(=C1)C(C)(C)C)C(C)(C)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for CGP 7930

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	ethanol	29.25	100
	DMSO	29.25	100

Preparing Stock Solutions for CGP 7930

The following data is based on the product molecular weight 292.46.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.42 mL	17.10 mL	34.19 mL
5 mM	0.68 mL	3.42 mL	6.84 mL
10 mM	0.34 mL	1.71 mL	3.42 mL
50 mM	0.07 mL	0.34 mL	0.68 mL

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References for CGP 7930

References are publications that support the biological activity of the product.

Hannan CGP7930 - An allosteric modulator of GABA_BRs, GABA_ARs and inwardly-rectifying potassium channels. Neuropharmacology 2023 PMID: 37422181
Liang The GABA_B receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology 2006 PMID: 16406445
Urwyler Positive allosteric modulation of native and recombinant γ-aminobutyric acid_B receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol.Pharmacol. 2001 PMID: 11641424
Chen Differential modulation by the GABA_B receptor allosteric potentiator 2,6-Di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)-phenol (CGP7930) of synaptic transmission in the rat hippocampal CA1 area. J.Pharmacol.Exp.Ther. 2006 PMID: 16507713