产品说明书

Lixivaptan

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Chemical Structure| 168079-32-1 同义名 : WAY-VPA 985;VPA-985;CRTX 080
CAS号 : 168079-32-1
货号 : A776512
分子式 : C27H21ClFN3O2
纯度 : 99%+
分子量 : 473.926
MDL号 : MFCD00937905
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：
生物活性
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].
临床研究
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 - -
实验方案
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
参考文献

[1]Albright JD, Reich MF, Delos Santos EG, Dusza JP, Sum FW, Venkatesan AM, Coupet J, Chan PS, Ru X, Mazandarani H, Bailey T. 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors. J Med Chem. 1998 Jul 2;41(14):2442-4

[2]Ghali JK, Zmily HD, Farah JO, Daifallah S. Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia. IDrugs. 2010 Nov;13(11):782-92

[3]Martinez-Castelao A. Lixivaptan (American Home Products). Curr Opin Investig Drugs. 2001 Apr;2(4):525-30