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CAS No.: 168079-32-1

Lixivaptan/利伐普坦 Catalog No. CSN21908

Synonyms: VPA-985;WAY-VPA 985;VPA-985, WAY-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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靶点选择性

生物活性

实验方案

技术信息

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 ... more >> 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 Collapse <<
NCT00578695	Hyponatremia	Phase 3	Completed	-	-
NCT00660959	Hyponatremia With Normal Extra... more >>cellular Fluid Volume Collapse <<	Phase 3	Completed	-	-

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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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1100 mL
- 10.5502 mL
- 21.1003 mL
- 5 mM
- 0.4220 mL
- 2.1100 mL
- 4.2201 mL
- 10 mM
- 0.2110 mL
- 1.0550 mL
- 2.1100 mL

技术信息

CAS号

168079-32-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H21ClFN3O2

运输

蓝冰

分子量

473.93

别名

VPA-985;WAY-VPA 985;VPA-985, WAY-VPA 985;CRTX-080

溶解度

DMSO	165.0 mg/mL (348.2 mM)
Water	insoluble

动物实验配方

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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 ... more >> 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 Collapse <<
NCT00578695	Hyponatremia	Phase 3	Completed	-	-
NCT00660959	Hyponatremia With Normal Extra... more >>cellular Fluid Volume Collapse <<	Phase 3	Completed	-	-
NCT00876798	Euvolemic Hyponatremia	Phase 3	Completed	-	-
NCT00675701	Healthy	Phase 1	Completed	-	United States, Texas ... more >> Research Site 1 Austin, Texas, United States, 78744 Collapse <<
NCT00876876	Hypervolemic Hyponatremia	Phase 3	Withdrawn(Created Extension st... more >>udy - This study was no longer feasible) Collapse <<	December 2010	-
NCT03717181	Polycystic Kidney	Phase 2	Not yet recruiting	March 31, 2020	-
NCT03487913	Autosomal Dominant Polycystic ... more >>Kidney Disease Collapse <<	Phase 2	Recruiting	June 2019	United States, California ... more >> Palladio Biosciences Clinical Site Recruiting Los Angeles, California, United States, 90022 Contact: Manaf Al-Sudaney 323-725-0051 msudaney@amrionline.net United States, Florida Palladio Biosciences Clinical Site Recruiting Jacksonville, Florida, United States, 32216 Contact: Richard Smith 904-730-0101 rsmith@encoredocs.com Contact: Sharon Smith 904-730-0166 ssmith@encoredocs.com Palladio Biosciences Clinical Site Recruiting Miami, Florida, United States, 33155 Contact: Luis E Sanchez 305-222-0155 lsanchez@healthandliferesearch.com Palladio Biosciences Clinical Site Recruiting Miami, Florida, United States, 33155 Contact: Maida Ramallo 305-667-1080 maida.crc@gmail.com Palladio Biosciences Clinical Site Not yet recruiting Miami, Florida, United States, 33165 Contact: Yudit Cabanes 786-615-2861 yc.mediclear@gmail.com Palladio Biosciences Clinical Site Recruiting Palmetto Bay, Florida, United States, 33157 Contact: Omar Orama 786-675-9452 omarorama.imrc@gmail.com Palladio Biosciences Clinical Site Not yet recruiting Tampa, Florida, United States, 33612 Contact: Cassie Miller 813-873-1016 cassiemiller@genesisclinicaltrials.com United States, Missouri Palladio Biosciences Clinical Site Recruiting Kansas City, Missouri, United States, 64111 Contact: Serine Alfaress 816-756-1222 serine@crckcmo.com United States, New York Palladio Biosciences Clinical Site Recruiting Laurelton, New York, United States, 11413 Contact: Ahmed Uddin 718-276-1264 auddin@scottresearch.org United States, Utah Palladio Biosciences Clinical Site Recruiting Salt Lake City, Utah, United States, 84115 Contact: Tiffany Herndon 801-747-9186 ukrinephrology@gmail.com Collapse <<
NCT01055912	Congestive Heart Failure	Phase 2	Completed	-	-

Lixivaptan/利伐普坦 Catalog No. CSN21908

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