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SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
| Molecular Weight | 703.87 |
| Formula | C42H49N5O5 |
| CAS Number | 512784-93-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) |
| 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. |
| L-371,257
L-371,257 is a potent and selective oxytocin receptor antagonist. |
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