512784-93-9
512784-93-9 structure
- Name: SRX246
- Chemical Name: SRX246
- CAS Number: 512784-93-9
- Molecular Formula: C42H49N5O5
- Molecular Weight: 703.87
- Catalog: Signaling Pathways GPCR/G Protein Vasopressin Receptor
- Create Date: 2020-01-23 16:28:51
- Modify Date: 2024-01-16 18:22:36
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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 is under development for the treatment of stress-related disorders[1].
| Name | SRX246 |
|---|
| Description | 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 is under development for the treatment of stress-related disorders[1]. |
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| Related Catalog | |
| Target |
Ki: 0.3 nM (human vasopressin 1a receptor)[1] |
| In Vivo | SRX246 (2 mg/kg; i.v.) treatment shows that the Cmax, AUC0-∞ and t1/2 values are 953 ng/mL, 1141 ng ▪h/mL, and 6.02 hours, respectively, in plasma pharmacokinetics. Following an oral administration (dose 20 mg/kg), The Cmax, AUC0-∞ and t1/2 values are 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively[1]. Animal Model: Male Sprague-Dawley rats[1] Dosage: 2 mg/kg (20 mg/kg for p.o.) Administration: i.v. (Pharmacokinetic Analysis) Result: Following i.v. administration, the plasma concentration declined steadily with a half-life (t1/2) of 6 hours. The Cmax and AUC0-∞ values are 953 ng/mL, 1141 ng ▪h/mL, 6.02 hours. Following an oral administration, the Cmax, AUC0-∞ and t1/2 values 98.4 ng/mL, 624 ng ▪h/mL and 2.38 hours, respectively. |
| References |
| Molecular Formula | C42H49N5O5 |
|---|---|
| Molecular Weight | 703.87 |
| Storage condition | 2-8°C |