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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)
Biological Activity for SR 49059
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.
Compound Libraries for SR 49059
SR 49059 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SR 49059
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SR 49059
| 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 620.5. 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.
| 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 |
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Product Datasheets for SR 49059
References for SR 49059
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for SR 49059, please let us know.
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Keywords: SR 49059, SR 49059 supplier, Selective, orally, active, vasopressin, V1a, receptor, antagonists, V2, Receptors, SR49059, Relcovaptan, Vasopressin, 2310, Tocris Bioscience
6 Citations for SR 49059
Citations are publications that use Tocris products. Selected citations for SR 49059 include:
Xiao et al (2018) OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons. Elife 7 PMID: 29676731
Manaenko et al (2011) Post-treatment with SR49059 improves outcomes following an intracerebral hemorrhagic stroke in mice. BMC Neurosci 111 191 PMID: 21725754
Xiao et al (2017) Biased OXTergic Modulation of Midbrain DA Systems. Neuron 95 368 PMID: 28669546
Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Acta Neurochir Suppl 34 852 PMID: 24517977
Manaenko et al (2011) Arginine-vasopressin V1a receptor inhibition improves neurologic outcomes following an intracerebral hemorrhagic brain injury. Neurochem Int 58 542 PMID: 21256175
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
Do you know of a great paper that uses SR 49059 from Tocris? Please let us know.
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Literature in this Area
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Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.