SR 49059
Tocris Bioscience, part of Bio-Techne | Catalog # 2310
Selective, orally active vasopressin V1A receptor antagonist
Key Product Details
Description
Selective, orally active vasopressin V1A receptor antagonist
Alternative Names
Relcovaptan
Product Description
SR 49059 is a 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.Product Specifications
Molecular Weight
620.50
Formula
C28H27Cl2N3O7S
Storage
Store at +4°C
Purity
≥98% (HPLC)
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
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.61 | 30 |
Preparing Stock Solutions
for SR 49059
The following data is based on the product molecular weight 620.50
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.3 mM | 5.37 mL | 26.86 mL | 53.72 mL |
| 1.5 mM | 1.07 mL | 5.37 mL | 10.74 mL |
| 3 mM | 0.54 mL | 2.69 mL | 5.37 mL |
| 15 mM | 0.11 mL | 0.54 mL | 1.07 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Tahtaoui 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. 2003 PMID: 12869559
- Serradeil-Le Gal Binding of [3H]SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem.Biophys.Res.Comm.
- Serradeil-Le Gal Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. J.Clin.Invest. 1993 PMID: 8392086
Product Specific Notices for SR 49059
For research use only
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