CGP 55845 hydrochloride

Name: CGP 55845 hydrochloride
Brand: Tocris Bioscience
SKU: 1248
Rating: 5 (2 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1248

(2)

Citations (123)

COA / SDS

Potent and selective GABAB antagonist

Key Product Details

Description:	Potent and selective GABA_B antagonist
Chemical Name:	(2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	438.71

View Full Technical Details for CGP 55845 hydrochloride

Technical Data
Citations / Reviews (2)

Biological Activity for CGP 55845 hydrochloride

CGP 55845 hydrochloride is a potent, selective GABA_B receptor antagonist (IC₅₀ = 5 nM) that prevents agonist binding (pK_i = 8.35) and inhibits GABA and glutamate release (pEC₅₀ values are 8.08 and 7.85 respectively). Inhibits GABA_B responses to baclofen (IC₅₀ = 130 nM in an isoproterenol assay) and potentiates the hypoglycemic response to glucose in vitro.

Licensing Information

Sold with the permission of Novartis Pharma AG

Compound Libraries for CGP 55845 hydrochloride

CGP 55845 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for CGP 55845 hydrochloride

M. Wt	438.71
Formula	C₁₈H₂₂Cl₂NO₃P.HCl
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	149184-22-5
PubChem ID	5311042
InChi Key	ZODSPDOOCZZEIM-BBRMVZONSA-N
Smiles	Cl.C[C@H](NC[C@H](O)CP(O)(=O)CC1=CC=CC=C1)C1=CC=C(Cl)C(Cl)=C1

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 55845 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	43.87	100 with gentle warming

Preparing Stock Solutions for CGP 55845 hydrochloride

The following data is based on the product molecular weight 438.71.

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	2.28 mL	11.40 mL	22.79 mL
5 mM	0.46 mL	2.28 mL	4.56 mL
10 mM	0.23 mL	1.14 mL	2.28 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

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References for CGP 55845 hydrochloride

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

Froestl Potent, orally active GABA_B receptor antagonists. Pharmacol.Rev.Comm.
Zhang Neurotransmitter mechanisms mediating low-glucose signalling in cocultures and fresh tissue slices of rat carotid body. J.Physiol. 2007 PMID: 17124268
Waldmeier GABA and glutamate release affected by GABA_B receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors. Br.J.Pharmacol. 1994 PMID: 7889310
Salah and Perkins Effects of subtype-selective group I mGluR antagonists on synchronous activity induced by 4-aminopyridine/CGP 55845 in adult guinea pig hippocampal slices. Neuropharmacology 2008 PMID: 18538357
Deisz The GABA_B antagonist CGP 55845A reduces presynaptic GABA₁ actions in neurons of the rat in vitro. Neuroscience 1999 PMID: 10501448
Cunninghan and Enna Evidence for pharmacologically distinct GABA_B receptors associated with cAMP production in rat brain. Brain Res. 1996 PMID: 8782915