GR 127935 hydrochloride

Pricing Availability   Qty

Save up to 40% on RUO Reagents with BIOSPRING24 (see details)

Description: Potent and selective 5-HT1B and 5-HT1D 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)
Citations (8)
Literature (1)

Biological Activity for GR 127935 hydrochloride

GR 127935 hydrochloride is a potent and selective 5-HT1B/1D receptor antagonist (pKi values are 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptors). Displays > 100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C 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
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 Data for GR 127935 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Product Datasheets for GR 127935 hydrochloride

Certificate of Analysis / Product Datasheet
Select another batch:

References for GR 127935 hydrochloride

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

Clitherow et al (1994) Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzalides as the first selective 5-HT1D antagonists. J.Med.Chem. 37 2253 PMID: 8057272

De Vries et al (1996) Blockade of porcine carotid vascular response to sumatr. by GR 127935, a selective 5-HT1D receptor antagonist. Br.J.Pharmacol. 118 85 PMID: 8733580

Knobelman et al (2001) Genetic regulation of extracellular serotonin by 5-hydroxytryptamine1A and 5-hydroxytryptamine1B autoreceptors in different brain regions of the mouse. J.Pharmacol.Exp.Ther. 298 1083 PMID: 11504805

If you know of a relevant reference for GR 127935 hydrochloride, please let us know.

View Related Products by Target

View Related Products by Product Action

View all 5-HT1D Receptor Antagonists

Keywords: GR 127935 hydrochloride, GR 127935 hydrochloride supplier, Potent, selective, 5-HT1B/1D, antagonist, Serotonin, Receptors, GR127935, hydrochloride, 5-HT1D, 5-HT1B, 1477, Tocris Bioscience

8 Citations for GR 127935 hydrochloride

Citations are publications that use Tocris products. Selected citations for GR 127935 hydrochloride include:

Li et al (2017) Pericytes impair capillary blood flow and motor function after chronic spinal cord injury. Nat Med 23 733 PMID: 28459438

Masterson and Durham (2010) DHE repression of ATP-mediated sensitization of trigeminal ganglion neurons. Headache 50 1424 PMID: 20561068

Akerman et al (2013) Endocannabinoids in the brainstem modulate dural trigeminovascular nociceptive traffic via CB1 and "triptan" receptors: implications in migraine. J Neurosci 33 14869 PMID: 24027286

Wei et al (2010) JNK regulates serotonin-mediated proliferation and migration of pulmonary artery smooth muscle cells. Am J Physiol Lung Cell Mol Physiol 298 L863 PMID: 20228179

Do you know of a great paper that uses GR 127935 hydrochloride from Tocris? Please let us know.

Reviews for GR 127935 hydrochloride

There are currently no reviews for this product. Be the first to review GR 127935 hydrochloride and earn rewards!

Have you used GR 127935 hydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

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.

5-HT Receptors Scientific Review

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.