Catalog Number: 2310
Alternate Names: Relcovaptan
Chemical Name: (2S)-1-[[(2R,3S)-5-Chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-2-pyrrolidinecarboxamide
Biological Activity
Potent and selective non-peptide vasopressin V1A receptor antagonist; devoid of agonist activity. Displays high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1 - 6.3 nM) V1A receptors. Potently antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.
Technical Data
  • M.Wt:
    620.5
  • Formula:
    C28H27Cl2N3O7S
  • Solubility:
    Soluble to 30 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    150375-75-0
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors.
    Serradeil-Le Gal et al.
    J.Clin.Invest., 1993;92:224
  2. Identification of the binding sites of the SR 49059 nonpeptide antagonist into the V1a vasopressin receptor using sulfydryl-reactive ligands and cysteine mutants as chemical sensors.
    Tahtaoui et al.
    J.Biol.Chem., 2003;278:40010
  3. Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes.
    Serradeil-Le Gal et al.
    Biochem.Biophys.Res.Comm., 1994;199:353
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SR 49059 include:

3 Citations: Showing 1 - 3
Filter your results:

  1. Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress.
    Authors: Faraco Et al.
    Acta Neurochir Suppl 2014;34:852
  2. Arginine vasopressin enhances cell survival via a G protein-coupled receptor kinase 2/β-arrestin1/extracellular-regulated kinase 1/2-dependent pathway in H9c2 cells.
    Authors: Zhu Et al.
    Mol Pharmacol 2013;84:227
  3. Post-treatment with SR49059 improves outcomes following an intracerebral hemorrhagic stroke in mice.
    Authors: Manaenko Et al.
    BMC Neurosci 2011;111:191

Have you used SR 49059?

Submit a review and receive a $25US/€18/£15/$25CAN amazon gift card if you include an image - $10US/€7/£6/$10CAN Amazon card for reviews without an image. Limited to verified customers in USA, Canada and Europe.

Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details

Note:

Contact Information

Calculators

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

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

R&D Systems Guarantee

or select another batch: 

Feedback

Customer Information