| CAS NO: | 512784-93-9 |
| 包装 | 价格(元) |
| 5mg | 询价 |
| 10mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| Cas No. | 512784-93-9 |
| Canonical SMILES | O=C(N1CCC(N2CCCCC2)CC1)C[C@H](C(N[C@@H](C3=CC=CC=C3)C)=O)N4[C@@H]([C@H](N5[C@@H](C6=CC=CC=C6)COC5=O)C4=O)/C=C/C7=CC=CC=C7 |
| 分子式 | C42H49N5O5 |
| 分子量 | 703.87 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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]. 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] [1]. Guillon CD, et al. Azetidinones as vasopressin V1a antagonists. Bioorg Med Chem. 2007 Mar 1;15(5):2054-80. [2]. Fabio KM, et al. Pharmacokinetics and metabolism of SRX246: a potent and selective vasopressin 1a antagonist. J Pharm Sci. 2013 Jun;102(6):2033-2043. |
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