CGP 55845 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 1248
Potent and selective GABAB antagonist
Key Product Details
Description
Potent and selective GABAB antagonist
Product Description
CGP 55845 hydrochloride is a potent, selective GABAB receptor antagonist (IC50 = 5 nM) that prevents agonist binding (pKi = 8.35) and inhibits GABA and glutamate release (pEC50 values are 8.08 and 7.85 respectively). Inhibits GABAB 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 AGProduct Specifications
Molecular Weight
438.71
Formula
C18H22Cl2NO3P.HCl
Storage
Store at RT
Purity
≥98% (HPLC)
Chemical Name
(2S)-3-[[(1S)-1-(3,4-Dichlorophenyl)ethyl]amino-2-hydroxypropyl](phenylmethyl)phosphinic acid hydrochloride
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all affect the solvent volumes required to prepare stock solutions.
| 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Froestl Potent, orally active GABAB 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 GABAB 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 GABAB 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 GABAB receptors associated with cAMP production in rat brain. Brain Res. 1996 PMID: 8782915
Product Specific Notices for CGP 55845 hydrochloride
For research use only
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