|1-(2,2-二氟-1,3-苯并二氧戊环-5-基)-N-[1-[(2R)-2,3-二羟基丙基]-6-氟-2-(2-羟基-1,1-二甲基乙基)-1H-吲哚-5-基]-环丙烷甲酰胺|CsnPharm

CAS No.: 1152311-62-0

Tezacaftor Catalog No. CSN15718

Synonyms: VX-661

VX-661 is a F508del CFTR corrector and is believed to help CFTR protein reach the cell surface.

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实验方案

技术信息

生物活性

描述Cystic fibrosis is caused by a reduced quantity or function of cystic fibrosis transmembrane conductance regulator (CFTR) protein, owing to mutations in CFTR. VX-661 is a first-generation CFTR corrector that has shown enhanced CFTR function and improved lung function in a phase 2 clinical trial involving patients who were homozygous for the Phe508del mutation or heterozygous for the Phe508del and G551D mutations ^[3]. The combination of VX-445 (2 μM) and VX-661 (18 μM) increased levels of mature CFTR protein and led to an increase in human bronchial epithelial cells from Phe508del–MF (a minimal-function mutation) and Phe508del–Phe508del (the Phe508del CFTR mutation) donors ^[4]. All doses of [VX-659-VX-661-ivacaftor] resulted in significant improvement in the percentage of predicted FEV₁ (forced expiratory volume in 1 second) as compared with the respective within-group baseline values at day 29 in patients with Phe508del-MF or Phe508del-Phe508del genotypes ^[5].
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
NCT03447249	Cystic Fibrosis	Phase 3	Active, not recruiting	April 16, 2019	-
NCT03460990	Cystic Fibrosis	Phase 3	Completed	-	-
NCT03447262	Cystic Fibrosis	Phase 3	Enrolling by invitation	April 24, 2021	-

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
- 1.9212 mL
- 9.6062 mL
- 19.2124 mL
- 5 mM
- 0.3842 mL
- 1.9212 mL
- 3.8425 mL
- 10 mM
- 0.1921 mL
- 0.9606 mL
- 1.9212 mL

技术信息

CAS号

1152311-62-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H27F3N2O6

运输

蓝冰

分子量

520.50

别名

VX-661

溶解度

DMSO	500.0 mg/mL (960.6 mM)
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	52 mg/mL	suspension

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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

NCT03447249	Cystic Fibrosis	Phase 3	Active, not recruiting	April 16, 2019	-
NCT03460990	Cystic Fibrosis	Phase 3	Completed	-	-
NCT03447262	Cystic Fibrosis	Phase 3	Enrolling by invitation	April 24, 2021	-
NCT03227471	Cystic Fibrosis	Phase 1 Phase 2	Completed	-	-
NCT03525574	Cystic Fibrosis	Phase 3	Enrolling by invitation	June 2021	-
NCT03224351	Cystic Fibrosis	Phase 2	Completed	-	-
NCT03525548	Cystic Fibrosis	Phase 3	Active, not recruiting	March 2019	-
NCT03029455	Cystic Fibrosis	Phase 1	Completed	-	United Kingdom ... more >> Birmingham, United Kingdom Cambridge, United Kingdom Exeter, United Kingdom Glasgow, United Kingdom Leeds, United Kingdom Liverpool, United Kingdom London, United Kingdom Manchester, United Kingdom Newcastle upon Tyne, United Kingdom Southampton, United Kingdom Collapse <<
NCT03537651	Cystic Fibrosis	Phase 3	Enrolling by invitation	December 2020	-
NCT03633526	Cystic Fibrosis	Phase 3	Recruiting	January 2020	United States, Colorado ... more >> Children's Hospital Colorado Recruiting Aurora, Colorado, United States, 80045 United States, Illinois Ann & Robert Lurie Children's Hospital of Chicago Recruiting Chicago, Illinois, United States, 60611 United States, Missouri The Children's Mercy Hospital Recruiting Kansas City, Missouri, United States, 64108 United States, North Carolina Clinical Research of Charlotte Recruiting Charlotte, North Carolina, United States, 28277 United States, Oregon Oregon Health & Science University Recruiting Portland, Oregon, United States, 97239 United States, Texas Texas Children's Hospital Recruiting Houston, Texas, United States, 77030 Collapse <<
NCT03691779	Cystic Fibrosis	Phase 3	Recruiting	January 2020	United States, California ... more >> Children's Hospital of Orange County Recruiting Orange, California, United States, 92868 United States, Massachusetts Boston Children's Hospital Recruiting Boston, Massachusetts, United States, 02115 United States, Minnesota Children's Respiratory and Critical Care Specialists, P.A., Children's Hospitals and Clinics of Minnesota Recruiting Minneapolis, Minnesota, United States, 55404 United States, New York Northwell Health- Long Island Jewish Medical Center Recruiting New Hyde Park, New York, United States, 11040 United States, Ohio Rainbow Babies and Children's Hospital/University Hospitals Cleveland Medical Center Recruiting Cleveland, Ohio, United States, 44106 Nationwide Children's Hospital Recruiting Columbus, Ohio, United States, 43205 Collapse <<
NCT03768089	Cystic Fibrosis	Phase 1 Phase 2	Recruiting	March 2019	Netherlands ... more >> Academic Medical Center Recruiting Amsterdam, Netherlands PRA Health Sciences Onderzoekscentrum UMCG Recruiting Groningen, Netherlands United Kingdom The Medicines Evaluation Unit Recruiting Manchester, United Kingdom Collapse <<
NCT03525444	Cystic Fibrosis	Phase 3	Active, not recruiting	August 2019	-
NCT02951182	Cystic Fibrosis	Phase 2	Completed	-	-
NCT03486236	Cystic Fibrosis	Phase 1	Completed	-	United Kingdom ... more >> The Medicines Evaluation Unit Manchester, United Kingdom Collapse <<
NCT02951195	Cystic Fibrosis	Phase 2	Completed	-	United States, Alabama ... more >> Birmingham, Alabama, United States United States, California La Jolla, California, United States Los Angeles, California, United States United States, Florida Orlando, Florida, United States United States, Illinois Chicago, Illinois, United States Peoria, Illinois, United States United States, Missouri Saint Louis, Missouri, United States United States, North Carolina Chapel Hill, North Carolina, United States United States, Ohio Akron, Ohio, United States Cleveland, Ohio, United States United States, Oregon Portland, Oregon, United States United States, Pennsylvania Philadelphia, Pennsylvania, United States United States, South Carolina Charleston, South Carolina, United States United States, Texas Fort Worth, Texas, United States Houston, Texas, United States United States, Wisconsin Madison, Wisconsin, United States Collapse <<
NCT02508207	Cystic Fibrosis	Phase 2	Completed	-	United States, Alabama ... more >> Birmingham, Alabama, United States United States, Indiana Indianapolis, Indiana, United States United States, Maryland Baltimore, Maryland, United States United States, North Carolina Chapel Hill, North Carolina, United States United States, Ohio Cincinnati, Ohio, United States Toledo, Ohio, United States United States, Pennsylvania Pittsburgh, Pennsylvania, United States Collapse <<
NCT02508207	-	-	Completed	-	-
NCT02412111	Cystic Fibrosis	Phase 3	Completed	-	-
NCT01531673	Cystic Fibrosis	Phase 2	Completed	-	-
NCT02070744	-	-	Completed	-	-
NCT02516410	Cystic Fibrosis	Phase 3	Completed	-	-
NCT02070744	Cystic Fibrosis	Phase 2	Completed	-	-
NCT02347657	-	-	Completed	-	-
NCT02730208	Cystic Fibrosis	Phase 2	Completed	-	Australia ... more >> Chermside, Australia Melbourne, Australia Nedlands, Australia New Lambton Heights, Australia Parkville SIC, Australia Randwick, Australia South Brisbane, Australia Subiaco, Australia Westmead, Australia Collapse <<
NCT01531673	-	-	Completed	-	-
NCT02015507	Cystic Fibrosis	Phase 1	Completed	-	-
NCT02347657	Cystic Fibrosis	Phase 3	Completed	-	-
NCT02516410	-	-	Completed	-	-
NCT02565914	Cystic Fibrosis	Phase 3	Enrolling by invitation	September 2019	-
NCT02953314	Cystic Fibrosis	Phase 3	Completed	-	-
NCT02392234	-	-	Completed	-	-
NCT02392234	Cystic Fibrosis	Phase 3	Completed	-	-

Tezacaftor Catalog No. CSN15718

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