CGP7930
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522380

CAS#: 57717-80-3

Description: CGP-7930 is a positive allosteric modulator at the GABAB receptor. It has anxiolytic effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and GHB, as well as reducing self-administration of ethanol and cocaine.


Chemical Structure

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CGP7930
CAS# 57717-80-3

Theoretical Analysis

MedKoo Cat#: 522380
Name: CGP7930
CAS#: 57717-80-3
Chemical Formula: C19H32O2
Exact Mass: 292.24023
Molecular Weight: 292.46
Elemental Analysis: C, 78.03; H, 11.03; O, 10.94

Size Price Shipping out time Quantity
10mg USD 330 2 Weeks
50mg USD 930 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-08. Prices are subject to change without notice.

CGP7930, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: CGP7930; CGP-7930; CGP 7930.

IUPAC/Chemical Name: 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethylpropyl)phenol

InChi Key: XLWJPQQFJNGUPA-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H32O2/c1-17(2,3)14-9-13(11-19(7,8)12-20)10-15(16(14)21)18(4,5)6/h9-10,20-21H,11-12H2,1-8H3

SMILES Code: OC1=C(C(C)(C)C)C=C(CC(C)(C)CO)C=C1C(C)(C)C

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

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 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Cedillo LN, Miranda F. Effects of co-administration of the GABAB receptor agonist baclofen and a positive allosteric modulator of the GABAB receptor, CGP7930, on the development and expression of amphetamine-induced locomotor sensitization in rats. Pharmacol Rep. 2013;65(5):1132-43. PubMed PMID: 24399709.

2: Mareš P, Tichá K, Mikulecká A. Anticonvulsant and behavioral effects of GABA(B) receptor positive modulator CGP7930 in immature rats. Epilepsy Behav. 2013 Jul;28(1):113-20. doi: 10.1016/j.yebeh.2013.04.011. Epub 2013 May 22. PubMed PMID: 23708148.

3: Ebenezer IS. Effects of intraperitoneal administration of the GABAB receptor positive allosteric modulator 2,6-di tert-butyl-4-(2-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) on food intake in non-deprived rats. Eur J Pharmacol. 2012 Sep 5;690(1-3):115-8. doi: 10.1016/j.ejphar.2012.05.021. Epub 2012 May 28. PubMed PMID: 22652431.

4: Mareš P. Anticonvulsant action of GABAB receptor positive modulator CGP7930 in immature rats. Epilepsy Res. 2012 Jun;100(1-2):49-54. doi: 10.1016/j.eplepsyres.2012.01.007. Epub 2012 Feb 15. PubMed PMID: 22341143.

5: Koek W, France CP, Cheng K, Rice KC. Effects of the GABAB receptor-positive modulators CGP7930 and rac-BHFF in baclofen- and γ-hydroxybutyrate-discriminating pigeons. J Pharmacol Exp Ther. 2012 May;341(2):369-76. doi: 10.1124/jpet.111.190975. Epub 2012 Feb 7. PubMed PMID: 22319197; PubMed Central PMCID: PMC3336808.

6: Brusberg M, Ravnefjord A, Martinsson R, Larsson H, Martinez V, Lindström E. The GABA(B) receptor agonist, baclofen, and the positive allosteric modulator, CGP7930, inhibit visceral pain-related responses to colorectal distension in rats. Neuropharmacology. 2009 Feb;56(2):362-7. doi: 10.1016/j.neuropharm.2008.09.006. Epub 2008 Sep 25. PubMed PMID: 18824012.

7: Parker DA, Marino V, Ong J, Puspawati NM, Prager RH. The CGP7930 analogue 2,6-di-tert-butyl-4-(3-hydroxy-2-spiropentylpropyl)-phenol (BSPP) potentiates baclofen action at GABA(B) autoreceptors. Clin Exp Pharmacol Physiol. 2008 Sep;35(9):1113-5. doi: 10.1111/j.1440-1681.2008.04948.x. Epub 2008 Apr 21. PubMed PMID: 18430050.

8: Jacobson LH, Cryan JF. Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents. Neuropharmacology. 2008 Apr;54(5):854-62. doi: 10.1016/j.neuropharm.2008.01.004. Epub 2008 Jan 13. PubMed PMID: 18328507.

9: Adams CL, Lawrence AJ. CGP7930: a positive allosteric modulator of the GABAB receptor. CNS Drug Rev. 2007 Fall;13(3):308-16. Review. PubMed PMID: 17894647.

10: Chen Y, Menendez-Roche N, Sher E. Differential modulation by the GABAB 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 Jun;317(3):1170-7. Epub 2006 Feb 28. PubMed PMID: 16507713.

11: Liang JH, Chen F, Krstew E, Cowen MS, Carroll FY, Crawford D, Beart PM, Lawrence AJ. The GABA(B) receptor allosteric modulator CGP7930, like baclofen, reduces operant self-administration of ethanol in alcohol-preferring rats. Neuropharmacology. 2006 Apr;50(5):632-9. Epub 2006 Jan 9. Erratum in: Neuropharmacology. 2006 Sep;51(3):692. PubMed PMID: 16406445.

12: Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, Froestl W, Gessa GL, Carai MA, Colombo G. Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur J Pharmacol. 2005 Nov 21;525(1-3):105-11. Epub 2005 Nov 14. PubMed PMID: 16289452.

13: Urwyler S, Gjoni T, Koljatić J, Dupuis DS. Mechanisms of allosteric modulation at GABAB receptors by CGP7930 and GS39783: effects on affinities and efficacies of orthosteric ligands with distinct intrinsic properties. Neuropharmacology. 2005 Mar;48(3):343-53. Epub 2005 Jan 25. PubMed PMID: 15721166.

14: Carai MA, Colombo G, Froestl W, Gessa GL. In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor. Eur J Pharmacol. 2004 Nov 19;504(3):213-6. PubMed PMID: 15541424.

15: Binet V, Goudet C, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L. Molecular mechanisms of GABA(B) receptor activation: new insights from the mechanism of action of CGP7930, a positive allosteric modulator. Biochem Soc Trans. 2004 Nov;32(Pt 5):871-2. Review. PubMed PMID: 15494037.

16: Binet V, Brajon C, Le Corre L, Acher F, Pin JP, Prézeau L. The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor. J Biol Chem. 2004 Jul 9;279(28):29085-91. Epub 2004 May 4. PubMed PMID: 15126507; PubMed Central PMCID: PMC2557059.

17: Onali P, Mascia FM, Olianas MC. Positive regulation of GABA(B) receptors dually coupled to cyclic AMP by the allosteric agent CGP7930. Eur J Pharmacol. 2003 Jun 20;471(2):77-84. PubMed PMID: 12818694.

18: Urwyler S, Mosbacher J, Lingenhoehl K, Heid J, Hofstetter K, Froestl W, Bettler B, Kaupmann K. Positive allosteric modulation of native and recombinant gamma-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 Nov;60(5):963-71. PubMed PMID: 11641424.