GR 127935 hydrochloride

Name: GR 127935 hydrochloride
Brand: Tocris Bioscience
SKU: 1477

Tocris Bioscience, part of Bio-Techne | Catalog # 1477

Citations (8)

COA / SDS

Potent and selective 5-HT1B and 5-HT1D antagonist

Key Product Details

Description:	Potent and selective 5-HT_1B and 5-HT_1D antagonist
Chemical Name:	N-[4-Methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-carboxamide hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	534.06

View Full Technical Details for GR 127935 hydrochloride

Technical Data
Citations

Biological Activity for GR 127935 hydrochloride

GR 127935 hydrochloride is a potent and selective 5-HT_1B/1D receptor antagonist (pK_i values are 8.5 for both guinea pig 5-HT_1D and rat 5-HT_1B receptors). Displays > 100-fold selectivity over 5HT_1A, 5-HT_2A, 5-HT_2C receptors and other receptor types. Centrally active following oral administration.

Licensing Information

Sold under license

Technical Data for GR 127935 hydrochloride

M. Wt	534.06
Formula	C₂₉H₃₁N₅O₃.HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	148642-42-6
PubChem ID	11497466
InChi Key	SRVVUYIJVBLEJI-UHFFFAOYSA-N
Smiles	Cl.COC1=C(C=C(NC(=O)C2=CC=C(C=C2)C2=CC=C(C=C2C)C2=NOC(C)=N2)C=C1)N1CCN(C)CC1

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 GR 127935 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	49.76	100

Preparing Stock Solutions for GR 127935 hydrochloride

The following data is based on the product molecular weight 534.06.

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	1.87 mL	9.36 mL	18.72 mL
5 mM	0.37 mL	1.87 mL	3.74 mL
10 mM	0.19 mL	0.94 mL	1.87 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

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References for GR 127935 hydrochloride

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

De Vries Blockade of porcine carotid vascular response to sumatr. by GR 127935, a selective 5-HT_1D receptor antagonist. Br.J.Pharmacol. 1996 PMID: 8733580
Knobelman Genetic regulation of extracellular serotonin by 5-hydroxytryptamine_1A and 5-hydroxytryptamine_1B autoreceptors in different brain regions of the mouse. J.Pharmacol.Exp.Ther. 2001 PMID: 11504805
Clitherow Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT_1D antagonists. J.Med.Chem. 1994 PMID: 8057272