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L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Decreases length of U-87MG cell projections induced by retinoic acid (Cat.No.0695). Orally active.
| Molecular Weight | 507.59 |
| Formula | C28H33N3O6 |
| CAS Number | 162042-44-6 |
| Solubility (25°C) | DMSO 5.08 mg/mL (with gentle warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Vasopressin Receptor Products |
|---|
| 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. |
| RG7713
RG7713 (RO5028442) is a highly effective and selective brain-osmotic vasopressin 1A (V1a) receptor antagonist with Ki values of 1 nM (hV1a) and 39 nM (mV1a). |
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