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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 加压素受体 / Lixivaptan/利伐普坦

Lixivaptan/利伐普坦 {[allProObj[0].p_purity_real_show]}

货号：A776512 同义名： WAY-VPA 985; VPA-985

Lixivaptan是一种口服活性且选择性的加压素V2受体拮抗剂，对人类和大鼠V2受体的IC50分别为1.2 nM和2.3 nM。

Lixivaptan/利伐普坦 化学结构 CAS号：168079-32-1
Lixivaptan/利伐普坦 化学结构
CAS号：168079-32-1
Lixivaptan/利伐普坦 3D分子结构
CAS号：168079-32-1
Lixivaptan/利伐普坦 化学结构 CAS号：168079-32-1
Lixivaptan/利伐普坦 3D分子结构 CAS号：168079-32-1
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Lixivaptan/利伐普坦 纯度/质量文件 产品仅供科研

货号：A776512 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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产品名称 Vasopressin receptor 1 ↓ Vasopressin receptor 2 ↓ 其他靶点 纯度
Conivaptan HCl ✔ 98%
Tolvaptan ++++

vasopressin receptor 2, IC50: 3 nM

 		97%
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。

Lixivaptan/利伐普坦 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].

Lixivaptan/利伐普坦 细胞实验

Cell Line
Concentration Treated Time Description References
MCD4 cells 100 nM 1 hour Lixivaptan completely abolished the effect of dDAVP on cAMP and prevented the dDAVP-induced increase in pS256-AQP2 levels, indicating its action as a V2R antagonist. Int J Mol Sci. 2019 Dec 26;21(1):183

Lixivaptan/利伐普坦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
PCK rats and Pkd1RC/RC mice PCK rats (model of autosomal recessive polycystic kidney disease) and Pkd1RC/RC mice (model of autosomal dominant polycystic kidney disease) Oral (added to diet) 0.5% PCK rats: 7 weeks; Pkd1RC/RC mice: 13 weeks To evaluate the effect of combined lixivaptan and R568 treatment on the progression of polycystic kidney disease. Results showed that the combined treatment significantly reduced kidney weight, cyst volume, and fibrosis volume. In PCK rats, kidney weight, cyst volume, and fibrosis volume were reduced by 20%, 49%, and 73%, respectively; in Pkd1RC/RC mice, they were reduced by 20%, 56%, and 69%, respectively. FASEB J. 2021 Oct;35(10):e21874
PCK rats PCK rat model Oral 0.5% (low dose) and 1% (high dose) 8 weeks To evaluate the effect of Lixivaptan on polycystic kidney disease development in the PCK rat model. Results showed that low dose Lixivaptan significantly reduced % kidney weight/body weight (26%), kidney cystic score (54%), kidney cAMP levels (23%), and plasma creatinine (13%), and increased urine output by 3-fold. High dose was less efficacious than low dose. Am J Nephrol. 2019;49(6):487-493

Lixivaptan/利伐普坦 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 - -

Lixivaptan/利伐普坦 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

Lixivaptan/利伐普坦 实验方案

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

Lixivaptan/利伐普坦 技术信息

CAS号168079-32-1
分子式C27H21ClFN3O2
分子量 473.93
SMILES Code O=C(NC1=CC=C(C(N2CC3=CC=CN3CC4=CC=CC=C24)=O)C(Cl)=C1)C5=CC(F)=CC=C5C
MDL No. MFCD00937905
别名 WAY-VPA 985; VPA-985; CRTX 080
运输蓝冰
InChI Key PPHTXRNHTVLQED-UHFFFAOYSA-N
Pubchem ID 172997
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

Tags: Lixivaptan | 168079-32-1 | VPA-985 | WAY-VPA 985 | VPA985 | VPA 985 | V2 Antagonist | GPCR/G Protein | Vasopressin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lixivaptan/利伐普坦 纯度/质量文件 | Lixivaptan/利伐普坦 亚型比较 | Lixivaptan/利伐普坦 生物活性 | Lixivaptan/利伐普坦 临床数据 | Lixivaptan/利伐普坦 参考文献 | Lixivaptan/利伐普坦 实验方案 | Lixivaptan/利伐普坦 技术信息

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