|2-(4-((5,6-二苯基吡嗪-2-基)(异丙基)氨基)丁氧基)-N-(甲磺酰基)乙酰胺|CsnPharm

CAS No.: 475086-01-2

Selexipag/赛乐西帕 Catalog No. CSN16825

Synonyms: NS-304;ACT-293987;Uptravi

NS-304 is an agonist of prostacyclin IP1 receptor with Ki of 260 nM. It is used for the treatment of pulmonary arterial hypertension.

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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NS-304 is an oral, selective prostacyclin IP1 receptor agonist (Ki values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP1-4, DP, FP, and TP receptors) for the treatment of pulmonary arterial hypertension.
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
NCT01347216	-	-	Recruiting	June 2020	Belgium ... more >> Dept. of Pneumology, University Recruiting Leuven, Belgium Contact: Marion Delcroix, MD, PhD Principal Investigator: Marion Delcroix, MD, PhD Germany DRK-Klinikum Köpenick Recruiting Berlin, Germany Contact: Christian Opitz, MD, PhD Principal Investigator: Christian Opitz, MD, PhD Lung Centre, University of Giessen Recruiting Giessen, Germany Contact: Ardeschir Ghofrani, MD, PhD Principal Investigator: Ardeschir Ghofrani, MD Sub-Investigator: Melanie Thamm, MD Department of Pulmology; Hannover Medical School Recruiting Hannover, Germany Contact: Marius M Hoeper Principal Investigator: Marius M Hoeper, MD, PhD Sub-Investigator: Karen Olsson, MD German Heart Centre Recruiting Munich, Germany Contact: Harald Kaemmerer, MD,. PhD Principal Investigator: Harald Kaemmerer, MD, PhD Ireland Mater Misericordiae Recruiting Dublin, Ireland Contact: Sean Gaine, MD, PhD Principal Investigator: Sean Gaine, MD, PhD Italy Department of Cardiovascular and Respiratory Sciences, University La Sapienza Recruiting Rome, Italy Contact: Dario Vizza, MD, PhD Principal Investigator: Dario Vizza, MD, PhD Switzerland Dept. for Rheumatology, University Hospital Recruiting Zurich, Switzerland Contact: Oliver Distler, MD, PhD Principal Investigator: Oliver Distler, MD, PhD Collapse <<
NCT03016468	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 2	Withdrawn(Business decision)	September 2018	-
NCT01389206	-	-	Completed	-	-

更多
参考文献

[1] Morrison K, Ernst R, et al. Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function. J Pharmacol Exp Ther. 2010 Oct;335(1):249-55.
[2] Kuwano K, Hashino A, et al. 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino] butoxy] -N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J Pharmacol Exp Ther. 2007 Sep;322(3):1181-8.

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
- 2.0136 mL
- 10.0680 mL
- 20.1361 mL
- 5 mM
- 0.4027 mL
- 2.0136 mL
- 4.0272 mL
- 10 mM
- 0.2014 mL
- 1.0068 mL
- 2.0136 mL

技术信息

CAS号

475086-01-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H32N4O4S

运输

蓝冰

分子量

496.62

别名

NS-304;ACT-293987;Uptravi;塞乐西帕

溶解度

DMSO	97.0 mg/mL (195.3 mM)
Water	Insoluble
Ethanol	47.0 mg/mL (94.6 mM)

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

NCT01347216	-	-	Recruiting	June 2020	Belgium ... more >> Dept. of Pneumology, University Recruiting Leuven, Belgium Contact: Marion Delcroix, MD, PhD Principal Investigator: Marion Delcroix, MD, PhD Germany DRK-Klinikum Köpenick Recruiting Berlin, Germany Contact: Christian Opitz, MD, PhD Principal Investigator: Christian Opitz, MD, PhD Lung Centre, University of Giessen Recruiting Giessen, Germany Contact: Ardeschir Ghofrani, MD, PhD Principal Investigator: Ardeschir Ghofrani, MD Sub-Investigator: Melanie Thamm, MD Department of Pulmology; Hannover Medical School Recruiting Hannover, Germany Contact: Marius M Hoeper Principal Investigator: Marius M Hoeper, MD, PhD Sub-Investigator: Karen Olsson, MD German Heart Centre Recruiting Munich, Germany Contact: Harald Kaemmerer, MD,. PhD Principal Investigator: Harald Kaemmerer, MD, PhD Ireland Mater Misericordiae Recruiting Dublin, Ireland Contact: Sean Gaine, MD, PhD Principal Investigator: Sean Gaine, MD, PhD Italy Department of Cardiovascular and Respiratory Sciences, University La Sapienza Recruiting Rome, Italy Contact: Dario Vizza, MD, PhD Principal Investigator: Dario Vizza, MD, PhD Switzerland Dept. for Rheumatology, University Hospital Recruiting Zurich, Switzerland Contact: Oliver Distler, MD, PhD Principal Investigator: Oliver Distler, MD, PhD Collapse <<
NCT03016468	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 2	Withdrawn(Business decision)	September 2018	-
NCT01389206	-	-	Completed	-	-
NCT02558231	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 3	Recruiting	December 31, 2019	-
NCT03278002	-	-	Recruiting	June 30, 2022	-
NCT01112306	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 3	Active, not recruiting	February 1, 2021	-
NCT02206204	Cardiodynamics ... more >> Safety Tolerability Pharmacokinetics Collapse <<	Phase 1	Completed	-	United States, Indiana ... more >> Covance Clinical Research Unit Evansville, Indiana, United States, 47710 Collapse <<
NCT01106014	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 3	Completed	-	-
NCT03078907	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 4	Recruiting	June 28, 2019	United States, California ... more >> LA Biomedical Research Institute Recruiting Torrance, California, United States, 90502 Contact: Ron Oudiz 310-222-3560 roudiz@labiomed.org United States, Georgia Northside Hospital Recruiting Atlanta, Georgia, United States, 30342 Contact: Paul Boyce 404-236-8113 paul.boyce@northside.com United States, Kentucky Kentuckiana Pulmonary Research Center Recruiting Louisville, Kentucky, United States, 40202 Contact: John McConnell 502-587-8000 Mcco3526@bellsouth.net United States, Massachusetts Tufts Medical Center Recruiting Boston, Massachusetts, United States, 02111 Contact: Nicholas Hill 617-636-4288 nhill@tuftsmedicalcenter.org United States, New York NYU Winthrop Hospital Recruiting Mineola, New York, United States, 11501 Contact: Shilpa DeSouza 516-663-9582 sdesouza@nyuwinthrop.org United States, North Carolina UNC Pulmonary Speciality Clinic Recruiting Chapel Hill, North Carolina, United States, 27599 Contact: Barbara LeVarge 919-966-2531 barbara_levarge@med.unc.edu United States, Ohio University of Cincinnati Recruiting Cincinnati, Ohio, United States, 45267-0564 Contact: Jean Elwing 513-558-2042 elwingj@ucmail.uc.edu Austria Krankenhaus der Elisabethinen Recruiting Linz, Austria, 4020 Contact: Regina Mascherbauer +43 732 7676 4916 regina.mascherbauer@elisabethinen.or.at Germany Charité Centrum Herz-, Kreislauf- und Gefäßmedizin, Campus Virchow-Klinikum Not yet recruiting Berlin, Germany, 13353 Contact: Frank Edelmann +49 30 450 55 37 31 Frank.edelmann@charite.de United Kingdom Papworth Hospital Recruiting Cambridge, United Kingdom, Cb23 3RE Contact: Joanna Pepke-Zaba +44 1480 83 05 41 joanna.pepkezaba@papworth.nhs.us Hammersmith Hospital Recruiting London, United Kingdom, W12 0HS Contact: Luke Howard +44 20 3313 31 71 l.howard@imperial.ac.uk Royal Hallamshire Hospital Recruiting Sheffield, United Kingdom, S10 2JF Contact: David Kiely +44 2073 52 81 21 david-kiely@sfh.nhs.uk Collapse <<
NCT02260557	Raynaud's Phenomenon Secondary... more >> to Systemic Sclerosis Collapse <<	Phase 2	Completed	-	France ... more >> Investigator Site Grenoble cedex, France, 38043 Investigator Site Lille Cedex, France, 59037 Investigator Site Nantes Cedex 1, France, 44093 Investigator Site Paris, France, 75679 Investigator Site Strasbourg, France, 67200 Germany Investigator Site Bad Nauheim, Germany, 61231 Investigator Site Berlin, Germany, 10117 Investigator Site Erlangen, Germany, 91054 Investigator Site Koln, Germany, 50937 Investigator Site Magdeburg, Germany, 39120 Investigator Site Mainz, Germany, 55131 United Kingdom Investigator Site Bath, United Kingdom, BA11RL Investigator Site Leeds, United Kingdom, LS74SA Investigator Site Liverpool, United Kingdom, L97AL Investigator Site London, United Kingdom, NW32QG Investigator Site Salford, United Kingdom, M55AP Collapse <<
NCT02770222	Healthy Subjects	Phase 1	Completed	-	Germany ... more >> Investigator Site Kiel, Germany, 24105 Collapse <<
NCT02206295	Bioequivalence	Phase 1	Completed	-	Netherlands ... more >> QPS Groningen, Netherlands, 9713 AG Collapse <<
NCT03689244	Chronic Thromboembolic Pulmona... more >>ry Hypertension Collapse <<	Phase 3	Not yet recruiting	April 1, 2022	-
NCT02471183	-	-	Completed	-	-
NCT03187678	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 3	Completed	-	United States, California ... more >> University of California San Diego Medical center - PULM VASCULAR DIV La Jolla, California, United States, 92037 United States, Massachusetts TUFTS New England Medical Center - PULM / CRITICAL CARE & SLEEP Boston, Massachusetts, United States, 02111-1552 United States, Ohio Cleveland Clin Foundation - Dept of Pulm & Critical Care Med Cleveland, Ohio, United States, 44195 United States, Texas University of Texas Southwestern Medical Center Dallas, Texas, United States, 75390-8550 Germany Universitätsklinikum Giessen und Marburg GmbH, Medizinische Klinik und Poliklinik II, Pneumologie Giessen, Germany, 35392 Universitätsmedizin Greifswald, Klinik und Poliklinik für Innere Medizin B Greifswald, Germany, 17475 Universitätsklinikum Hamburg-Eppendorf, II. Medizinische Klinik und Poliklinik, Pneumologie Hamburg, Germany, 20246 Universitätsklinikum Leipzig / Medizinischen Klinik und Poliklinik I, Pneumologie Leipzig, Germany, 04103 Collapse <<
NCT03492177	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 2	Recruiting	December 30, 2025	France ... more >> HOSP ARNAUD DE VILLENEUVE - PAED DEPT (Montpellier) Recruiting Montpellier, France, 34295 Contact: Principal Investigator + 33 4 67 33 67 33 p-amedro@chu-montpellier.fr HOSP NECKER _CARDIOLOGY PEDIATRY DEPT (Paris) Recruiting Paris, France, 75015 Contact: Principal Investigator +33 1 44 49 43 44 damien.bonnet@nck.aphp.fr HOSP DES ENFANTS_CARDIOLOGY DEPT (Toulouse Cedex 9) Recruiting Toulouse Cedex 9, France, 31059 Contact: Principal Investigator + 33 5 61 77 22 33 dulac.y@chu-toulouse.fr Hungary Gottsegen Gyorgy National Card Inst - Pediatric Card Recruiting Budapest, Hungary, 1096 Contact: Principal Investigator +36 1 215 1220 ablonczyl@kardio.hu Collapse <<
NCT02882425	Healthy Subjects	Phase 1	Completed	-	France ... more >> Investigator Site Rennes, France, 35042 Collapse <<
NCT02471183	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 3	Completed	-	United States, California ... more >> UCSD Medical Center -La Jolla La Jolla, California, United States UCSF Medical Center San Francisco, California, United States Harbor UCLA Medical Center Torrance, California, United States United States, Georgia Emory University Atlanta, Georgia, United States Piedmont Healthcare Research Institute Austell, Georgia, United States United States, Kentucky Kentuckiana Pulmonary Associates Louisville, Kentucky, United States United States, Michigan University of Michigan Health System Ann Arbor, Michigan, United States United States, Missouri Washington University School of Medicine Saint Louis, Missouri, United States United States, North Carolina Duke Unversity Durham, North Carolina, United States United States, Pennsylvania University of Pennsylvania Philadelphia, Pennsylvania, United States Allegheny General Hospital Pittsburgh, Pennsylvania, United States University of Pittsburgh Medical Center Health System Pittsburgh, Pennsylvania, United States United States, Texas UT Southwestern Dallas, Texas, United States Houston Methodist Hospital Houston, Texas, United States United States, Virginia Sentara Cardiovascular Research Instistute Norfolk, Virginia, United States Collapse <<
NCT02745860	Healthy Subjects	Phase 1	Completed	-	Germany ... more >> Investigator Site. Kiel, Germany, 24105 Collapse <<
NCT03496506	Healthy Subjects	Phase 1	Completed	-	Belgium ... more >> Clinical Pharmacology Unit (CPU) Merksem, Belgium, 2170 Collapse <<
NCT00993408	Pulmonary Arterial Hypertensio... more >>n Collapse <<	Phase 2	Completed	-	Austria ... more >> Medizinische Universitat Wien, Universitatsklinik fur Innere Medizin II, Kardiologie Vienna, Austria, 1090 Belgium Gasthuisberg University Hospital, Pneumology Leuven, Belgium, 3000 France Hopital Antoine Beclere, Pneumologie Paris, France Germany Department of Respiratory Medicine, Hannover Medical School Hannover, Germany, 30625 Hungary Semmelweis University, Clinic of Pulmonology Budapest, Hungary, H-1125 Italy Hospital Sant'Orsola Malpighi, Cardiology's Department Bologna, Italy, 40138 Poland Instytut Gruzilcy i Chorob Pluc, Klinika Chorob Wewnetrznych Klatki Piersiowej Warsaw, Poland, 01-138 United Kingdom Hammersmith Hospital London, United Kingdom, W12 0HS Collapse <<
NCT02791815	Healthy Subjects	Phase 1	Completed	-	France ... more >> Investigator Site Gieres, France, 38610 Collapse <<
NCT01106014	-	-	Completed	-	-

Selexipag/赛乐西帕 Catalog No. CSN16825

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