CGP 7930

Pricing Availability   Qty
Description: Positive allosteric modulator of GABAB receptors
Chemical Name: 3,5-bis(1,1-Dimethylethyl)-4-hydroxy-β,β-dimethyl-benzenepropanol
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (2)

Biological Activity for CGP 7930

CGP 7930 is a positive allosteric modulator of GABAA and GABAB receptors. Increases the potency and efficacy of GABA at both recombinant and native GABAB 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 GABAA 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 GABAA receptor currents by specific type-A receptor agonist Muscimol (EC50 = 2.0 μM). CGP7930 potentiates GABAA 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 GABAA 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 Data 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.42 mL 17.1 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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Product Datasheets for CGP 7930

Certificate of Analysis / Product Datasheet
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View Related Products by Product Action

View all GABAB Receptor Modulators

Keywords: CGP 7930, CGP 7930 supplier, Positive, modulators, GABAB, receptors, GABAA, receptor, PAM, CGP7930, GIRK, Inward, Rectifier, Potassium, Channels, Kir, Receptors, rectifier, 1513, Tocris Bioscience

3 Citations for CGP 7930

Citations are publications that use Tocris products. Selected citations for CGP 7930 include:

Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. PLoS One 5 10468 PMID: 26020477

Rondard et al (2008) Functioning of the dimeric GABA(B) receptor extracellular domain revealed by glycan wedge scanning. EMBO J 27 1321 PMID: 18388862

Tu et al (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J Neurosci 30 749 PMID: 20071540


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GABA Receptors Scientific Review

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.