货号:A776512 同义名: WAY-VPA 985;VPA-985
Lixivaptan is an orally active and selective vasopressin receptor V2 antagonist with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.
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产品名称 | Vasopressin receptor 1 ↓ ↑ | Vasopressin receptor 2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
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Conivaptan hydrochloride | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively[1]. Lixivaptan, is a non-peptide, selective vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia associated with heart failure. In preclinical studies, lixivaptan displayed competitive antagonist activity at V2 receptors in vitro, and increased urine volume and decreased urine osmolality in rats and dogs[2]. It selectively prevents vasopressin-dependent water resorption, increasing water excretion with low electrolyte loss [266993] and is selective towards the human V2 versus V1 receptors[3]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01056848 | - | Completed | - | United States, California ... 展开 >> Torrance Clinical Research Lomita, California, United States, 90717 United States, Florida Innovative Research of West Florida Clearewater, Florida, United States, 33756 Fleming Island Center for Clinical Research Fleming Island, Florida, United States, 32003 Jacksonville Center for Clinical Research Jacksonville, Florida, United States, 32216 United States, Missouri Millenium Psychiatric Associates, LLC Creve Cour, Missouri, United States, 63141 United States, Nebraska Internal Medical Associates of Grand Island, PC Grand Island, Nebraska, United States, 68803 收起 << | |
NCT00578695 | Hyponatremia | Phase 3 | Completed | - | - |
NCT00660959 | Hyponatremia With Normal Extra... 展开 >>cellular Fluid Volume 收起 << | Phase 3 | Completed | - | - |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.11mL 0.42mL 0.21mL |
10.55mL 2.11mL 1.06mL |
21.10mL 4.22mL 2.11mL |
CAS号 | 168079-32-1 |
分子式 | C27H21ClFN3O2 |
分子量 | 473.926 |
别名 | WAY-VPA 985;VPA-985;CRTX 080 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 145 mg/mL(305.95 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |