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SR 49059 is a potent and selective Arginine Vasopressin (AVP) V1a-receptor antagonist, with a Ki vaule of 1.4 nM. AVP is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes V1a, V1b, and V2. All belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF. SR 49059 has also shown initial positive results in the treatment of Raynaud′s disease, dysmenorrhoea, and tocolysis.
| Molecular Weight | 620.5 |
| Formula | C28H27Cl2N3O7S |
| CAS Number | 150375-75-0 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage | -20°C, sealed |
| Related Vasopressin Receptor Products |
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| Mozavaptan
Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V2 receptor antagonist with an IC50 of 14 nM. Mozavaptan shows ~85-fold selectivity for V2 receptor over V1 receptor (IC50 of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. |
| Tolvaptan
Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation. |
| Conivaptan hydrochloride
Conivaptan hydrochloride is a non-peptide vasopressin receptor antagonist, which can inhibit V1A receptor in rat liver and V2 receptor in kidney with Ki values of 0.48 and 3.04 nM, respectively. |
| Atosiban Acetate
Atosiban (RW22164; Tractocile) Acetate is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. |
| L-371,257
L-371,257 is a potent and selective oxytocin receptor antagonist. |
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