SR 49059

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Cat.No. 2310 - SR 49059 | C28H27Cl2N3O7S | CAS No. 150375-75-0
Description: Selective, orally active vasopressin V1A receptor antagonist
Alternative 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
Purity: ≥99% (HPLC)
Datasheet
Citations (3)
Literature

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.

Compound Libraries

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Technical Data

M. Wt 620.5
Formula C28H27Cl2N3O7S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 150375-75-0
PubChem ID 60943
InChI Key CEBYCSRFKCEUSW-NAYZPBBASA-N
Smiles O=S(C1=CC(OC)=C(OC)C=C1)(N2[C@@H]([C@@](N5CCC[C@H]5[C@@](N)=O)=O)[C@](C4=CC=CC=C4Cl)(O)C3=C2C=CC(Cl)=C3)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.61 30

Preparing Stock Solutions

The following data is based on the product molecular weight 620.5. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.61 mL 8.06 mL 16.12 mL
5 mM 0.32 mL 1.61 mL 3.22 mL
10 mM 0.16 mL 0.81 mL 1.61 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Serradeil-Le Gal et al (1993) Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. J.Clin.Invest. 92 224 PMID: 8392086

Tahtaoui et al (2003) 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. J.Biol.Chem. 278 40010 PMID: 12869559

Serradeil-Le Gal et al (1994) Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm. 199 353 PMID:


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Keywords: SR 49059, supplier, Selective, orally, active, vasopressin, V1a, receptor, antagonists, V2, Receptors, SR49059, Relcovaptan, Vasopressin, Receptors, Tocris Bioscience

3 Citations for SR 49059

Citations are publications that use Tocris products. Selected citations for SR 49059 include:

Manaenko et al (2011) Post-treatment with SR49059 improves outcomes following an intracerebral hemorrhagic stroke in mice. BMC Neurosci 111 191 PMID: 21725754

Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Acta Neurochir Suppl 34 852 PMID: 24517977

Zhu et al (2013) 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. Mol Pharmacol 84 227 PMID: 23690069


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