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
SR 49059 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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.
| 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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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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