V1a/V2 antagonist 1_product_DataBase

Bioactivity	V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice[1].
Invitro	V1a/V2 antagonist 1 (1 μM) 具有良好的的肝微粒体代谢稳定性，其 Clint (h/r/m) (μL/min/mg) 为15.9/36.9/ 27.1[1]。V1a/V2 antagonist 1 与 hERG 没有相互作用 (IC50：>30 μM)，PDR 值为 0.91 (VB-Caco-2 渗透性试验) [1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> V1a/V2 antagonist 1 相关抗体:
In Vivo	V1a/V2 antagonist 1 (0.1-3 mg/kg，口服，60 min 预处理) 显著抑制 Oxytocin (HY-17571) 诱发的小鼠抓挠行为[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
Formula	C25H26ClN5O3
Molar Mass	479.96
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Varró G, et al. Development of dual V1a/V2 antagonists containing triazolobenzazepine scaffold. Eur J Med Chem. 2024 Nov 28;283:117069.

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