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SR 49059
- Relcovaptan
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C28H27Cl2N3O7S
- MW: 620.5
Description
SR 49059 (Relcovaptan) is a highly potent and selective vasopressin V1A receptor antagonist. SR 49059 selectively blocks vasopressin-mediated V1A receptor signaling and has been extensively used as a pharmacological tool to investigate the physiological and pathological functions of the vasopressin V1A receptor.
The vasopressin V1A receptor is involved in vascular regulation, smooth muscle contraction, stress responses, social behavior, and neuroendocrine signaling. SR 49059 is a valuable research tool for studying vasopressin biology, GPCR pharmacology, cardiovascular physiology, and central nervous system function.
Key Features
- Highly potent and selective V1A receptor antagonist
- Ki value of 1.1-6.3 nM, with little to no affinity for V1B and V2, or oxytocin receptors.
- Acts as a full V1A antagonist, without demonstrating any intrinsic agonistic (stimulating) activity.
- Orally bioavailable, exhibiting a long duration of action in biological models.
- Useful for neuroendocrine and cardiovascular research
Applications
- Vasopressin receptor pharmacology
- V1A receptor signaling studies
- Cardiovascular and vascular biology research
- Stress response and neuroendocrine investigations
- GPCR and neuroscience research
More Information
| Parent CAS No. | 150375-75-0 |
|---|---|
| Chemical Name | (S)-1-[(2R,3S)-5-Chloro-3-(2-chloro-phenyl)-1-(3,4-dimethoxy-benzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl]-pyrrolidine-2-carboxylic acid amide |
| SMILES | [C@@H]1(C(=O)N2CCC[C@H]2C(=O)N)N(S(=O)(=O)C2=CC=C(OC)C(OC)=C2)C2=C(C=C(C=C2)Cl)[C@]1(O)C1C=CC=CC=1Cl |&1:0,7,32,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C28H27Cl2N3O7S/c1-39-23-12-10-17(15-24(23)40-2)41(37,38)33-21-11-9-16(29)14-19(21)28(36,18-6-3-4-7-20(18)30)25(33)27(35)32-13-5-8-22(32)26(31)34/h3-4,6-7,9-12,14-15,22,25,36H,5,8,13H2,1-2H3,(H2,31,34)/t22-,25-,28+/m0/s1 |
| InChiKey | CEBYCSRFKCEUSW-NAYZPBBASA-N |
| CID | 60943 |
| Short Description | V1A antagonist |
References
- Steinwall et al. The effect of relcovaptan (SR 49059), an orally active vasopressin V1a receptor antagonist, on uterine contractions in preterm labor. Gynecol Endocrinol. 2005 20(2), 104-9.
- Tahtaoui et al. 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, 278, 40010.
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