|3-((丁氧基)甲基) 5-甲基 4-(2,3-二氯苯基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸酯|CsnPharm

CAS No.: 167221-71-8

Clevidipine/丁酸氯维地平 Catalog No. CSN12960

Synonyms: rac-Clevidipine;Clevelox;Cleviprex

Clevidipine is a short-acting dihydropyridine calcium channel antagonist with IC50 of 7.1 nM, it's under development for treatment of perioperative hypertension.

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生物活性

描述Clevidipine is a short-acting dihydropyridine calcium channel antagonist. Clevidipine is an ultrashort-acting drug for rapid reduction of blood pressure by selectively acting on the L-type Ca2+ channels on arteriolar smooth muscle. The drug's ultrashort action in reducing the blood pressure is due to its rapid hydrolysis by blood and extravascular tissue esterases, which does not depend on hepato-renal metabolism and excretion^[3]. When myocytes were voltage-clamped with holding potential (VH) at -80 mV, 10 nM clevidipine decreased ICa at 0 mV by approximately 30%, but >50% when VH was -40 mV^[4]. Clevidipine is an endothelium-independent arterial vasodilator that offers a potential therapeutic option in the treatment of perioperative arterial graft vasospasm and/or hypertension^[2]. Clevidipine provided rapid BP control in patients with acute neurological injuries (including intracerebral haemorrhage, subarachnoid haemorrhage and acute ischaemic stroke), and was not associated with 'overshoot' in the vast majority of patients. Intravenous clevidipine was generally well tolerated and was usually associated with no reflex tachycardia or only very modest increases in heart rate^[5]. Clevidipine administration during initial medical management of aortic dissection showed similar efficacy compared to SNP (sodium nitroprusside) when used as adjunct therapy to esmolol^[6].
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
NCT01369147	Critical Illness	Phase 2	Suspended(The study has been h... more >>alted pending additional funding.) Collapse <<	October 2019	United States, Georgia ... more >> Emory University Hospital Atlanta, Georgia, United States, 30322 Collapse <<
NCT03719001	Vascular Diseases	Early Phase 1	Recruiting	October 1, 2020	United States, California ... more >> University of California San Francisco Recruiting San Francisco, California, United States, 94122 Contact: Pekka Talke, MD 415-476-8963 pekka.talke@ucsf.edu Contact: Pekka Talke, MD 415-476-8963 talkep@anesthesia.ucsf.edu Collapse <<
NCT01033370	Aortic Aneurysm ... more >> Aortic Disease Collapse <<	Phase 4	Terminated(Project lacked fund... more >>ing.) Collapse <<	-	United States, Texas ... more >> The Methodist Hospital Houston, Texas, United States, 77030 Collapse <<

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参考文献

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
- 2.1915 mL
- 10.9573 mL
- 21.9146 mL
- 5 mM
- 0.4383 mL
- 2.1915 mL
- 4.3829 mL
- 10 mM
- 0.2191 mL
- 1.0957 mL
- 2.1915 mL

技术信息

CAS号

167221-71-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H23Cl2NO6

运输

蓝冰

分子量

456.32

别名

rac-Clevidipine;Clevelox;Cleviprex;167221-71-8;氯维地平;丁酸氯维地平

溶解度

DMSO	120.0 mg/mL (263.0 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

NCT01369147	Critical Illness	Phase 2	Suspended(The study has been h... more >>alted pending additional funding.) Collapse <<	October 2019	United States, Georgia ... more >> Emory University Hospital Atlanta, Georgia, United States, 30322 Collapse <<
NCT03719001	Vascular Diseases	Early Phase 1	Recruiting	October 1, 2020	United States, California ... more >> University of California San Francisco Recruiting San Francisco, California, United States, 94122 Contact: Pekka Talke, MD 415-476-8963 pekka.talke@ucsf.edu Contact: Pekka Talke, MD 415-476-8963 talkep@anesthesia.ucsf.edu Collapse <<
NCT01033370	Aortic Aneurysm ... more >> Aortic Disease Collapse <<	Phase 4	Terminated(Project lacked fund... more >>ing.) Collapse <<	-	United States, Texas ... more >> The Methodist Hospital Houston, Texas, United States, 77030 Collapse <<
NCT00803634	Hypertension ... more >>Heart Failure Collapse <<	Phase 3	Completed	-	United States, Alabama ... more >> Jackson Hospital Montgomery, Alabama, United States, 36106 United States, California Centinela Hospital Inglewood, California, United States, 90301 United States, Louisiana Louisiana State University Health Sciences Center Baton Rouge, Louisiana, United States, 70805 Louisiana State University Health Sciences Center - Emergency Medicine New Orleans, Louisiana, United States, 70112 United States, Missouri Washington University School of Medicine St. Louis, Missouri, United States, 63110 United States, New York Stony Brook University and Medical Center Stony Brook, New York, United States, 11794 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio University of Cincinnati Cincinnati, Ohio, United States, 45267 The Cleveland Clinic Cleveland, Ohio, United States, 44195 France Hopial AP-HP Hotel-Dieu Paris, France, 75004 Hopital AP-HP La Pitie Sapetriere Paris, France, 75013 Hopital AP-HP Lariboisiere Urgencies-SMUR Paris, France, 75475 Germany Charité - Universitätsmedizin Berlin Berlin, Germany, 13353 Collapse <<
NCT00093262	Hypertension	Phase 3	Completed	-	United States, Alabama ... more >> Discovery Alliance - Mobile Infirmary Medical Center Mobile, Alabama, United States, 36602 United States, California Keck School of Medicine, University of Southern California Los Angeles, California, United States, 90033 Huntington Memorial Hospital Pasadena, California, United States, 91109 Stanford University School of Medicine Stanford, California, United States, 94305-5640 United States, Georgia Emory Hospital Atlanta, Georgia, United States, 30322 United States, Illinois Heart Care Research Foundation Blue Island, Illinois, United States, 60406 MacNeal Hospital Glencoe, Illinois, United States, 60022 United States, Kansas Wesley Medical Center Wichita, Kansas, United States, 67214 United States, Missouri St. Lukes Hospital Kansas City, Missouri, United States, 64111 United States, Montana International Heart Institute Missoula, Montana, United States, 59802 United States, New York Mt. Sinai Medical Center New York, New York, United States, 10029-6574 Columbia University - College of Physicians and Surgeons New York, New York, United States, 10032 United States, North Carolina Carolinas Medical Center Charlotte, North Carolina, United States, 28203 United States, Texas Discovery Alliance - Methodist Hospital / Diagnostic West Pavillion Houston, Texas, United States, 77030 United States, Wisconsin Medical College of Wisconsin VAMC - Milwaukee Milwaukee, Wisconsin, United States, 53295 Collapse <<
NCT00803634	-	-	Completed	-	-
NCT00093886	Hypertension	Phase 3	Completed	-	-
NCT00093925	Hypertension	Phase 3	Completed	-	United States, Alabama ... more >> Mobile Infirmary Medical Center Mobile, Alabama, United States, 36607 United States, Kansas Wesley Medical Center Wichita, Kansas, United States, 67214 United States, Louisiana Touro Infirmary New Orleans, Louisiana, United States, 70115 Ochsner Clinic Foundation New Orleans, Louisiana, United States, 70121 United States, New York Jack D. Weller Hospital Bronx, New York, United States, 10461 Montefiore Medical Center Bronx, New York, United States, 10467 Columbia University - College of Physicians and Surgeons New York, New York, United States, 10032 United States, Pennsylvania Hospital of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 United States, Virginia VA Medical Center McGuire Richmond, Virginia, United States, 23249 Collapse <<
NCT01042574	Hypertension ... more >>Intracranial Hemorrhage Subarachnoid Hemorrhage Collapse <<	Phase 4	Withdrawn	July 2013	United States, Tennessee ... more >> Methodist Healthcare, University Hospital Memphis, Tennessee, United States, 38104 Collapse <<
NCT00093249	Hypertension	Phase 3	Completed	-	United States, Alabama ... more >> Cardio-Thoracic Surgeons, PC Birmingham, Alabama, United States, 35213 United States, California St Vincent Medical Center Los Angeles, California, United States, 90057 United States, Florida Discovery Alliance - Hudson Hudson, Florida, United States, 34667 Discovery Alliance - Sacred Heart Hospital Pensacola, Florida, United States, 32503 United States, Georgia Atlanta VA Medical Center Atlanta, Georgia, United States, 30322 United States, Illinois MacNeal Hospital Berwyn, Illinois, United States, 60402 United States, North Carolina Wake Forest University School of Medicine Winston-Salem, North Carolina, United States, 27157 United States, Ohio The Christ Hospital, The Linder Clinical Trial Center Cincinnati, Ohio, United States, 45219 United States, Texas Memorial Herman Memorial City Hospital Houston, Texas, United States, 77024 Texas Heart Institute Houston, Texas, United States, 77030 Houston Northwest Medical Center Houston, Texas, United States, 77090 United States, Washington Swedish Hospital Medical Center Seattle, Washington, United States, 98104-1318 Collapse <<
NCT01645111	-	-	Completed	-	-
NCT00093912	Hypertension	Phase 3	Completed	-	-
NCT00978822	Subarachnoid Hemorrhage ... more >> Hypertension Collapse <<	Phase 2	Unknown	June 2010	United States, Michigan ... more >> Henry Ford Hospital Recruiting Detroit, Michigan, United States, 48202 Contact: Kathleen Wilson, Bsc, RN 313-916-3501 kwilso10@hfhs.org Principal Investigator: Panayiotis N Varelas, MD, PhD Sub-Investigator: Tamer Abdelhak, MD Collapse <<
NCT01645111	Neuromuscular Scoliosis	Phase 2 Phase 3	Completed	-	United States, Ohio ... more >> Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Collapse <<
NCT01121458	Hypertension, Pulmonary	Phase 4	Completed	-	United States, Texas ... more >> VA North Texas Health Care System Dallas, Texas, United States, 75216 Collapse <<
NCT00369837	Hypertension	Phase 3	Completed	-	United States, Alabama ... more >> Jackson Hospital Montgomery, Alabama, United States, 36106 United States, California VA Medical Center W. LA Los Angeles, California, United States, 90073 United States, District of Columbia The George Washington University Medical Center Washington, District of Columbia, United States, 20037 United States, Louisiana Louisiana State University Medical Center/Charity Hospital New Orleans, Louisiana, United States, 70118 Critical Care Research Center at Louisiana State University Health Sciences Center Shreveport, Louisiana, United States, 71103 United States, Maryland Good Samaritan Hospital Baltimore, Maryland, United States, 21239 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Ohio Metrohealth Medical Center Cleveland, Ohio, United States, 44109 The Cleveland Clinic Cleveland, Ohio, United States, 44195 The Toledo Hospital Toledo, Ohio, United States, 43606 United States, Oregon Providence Heart & Vascular Institute, d/b/a Providence St. Vincent Medical Center Portland, Oregon, United States, 97225 United States, Pennsylvania Hamot Shock Trauma Erie, Pennsylvania, United States, 16550 Pennsylvania Hospital Philadelphia, Pennsylvania, United States, 19107 United States, Texas The University of Texas Health Science Center Houston, Texas, United States, 77030 Collapse <<
NCT01526876	Hypertension	Phase 4	Withdrawn(Terminated by Sponso... more >>r) Collapse <<	-	-
NCT00799604	Hypertension	Phase 2	Completed	-	United States, Massachusetts ... more >> Massachusetts General Hospital, Harvard Medical School Boston, Massachusetts, United States, 02114 United States, Pennsylvania Hospital of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT00799604	-	-	Completed	-	-
NCT00666328	-	-	Completed	-	-
NCT01938547	Pediatric Perioperative Blood ... more >>Pressure Management Collapse <<	Phase 4	Suspended	December 2018	United States, California ... more >> Stanford Medical Center Stanford, California, United States, 94305 United States, Ohio Nationwide Children's Hospital Columbus, Ohio, United States, 43205 Collapse <<
NCT01910532	Hypertension	Phase 4	Withdrawn(Sponsor discontinued... more >> the research) Collapse <<	-	United States, Ohio ... more >> The Ohio State University Medical Center Columbus, Ohio, United States, 43210 Collapse <<
NCT00666328	Hypertension ... more >>Hemorrhage Collapse <<	Phase 3	Completed	-	United States, District of Col... more >>umbia Washington Hospital Center Washington, District of Columbia, United States, 20010-2975 United States, Hawaii The Queens Medical Center Honolulu, Hawaii, United States, 96813 United States, Maryland The John Hopkins Hospital Baltimore, Maryland, United States, 21287 United States, Massachusetts Maine Medical Center Portland, Massachusetts, United States, 04102 United States, Michigan Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, New York Columbia University Medical Center New York, New York, United States, 10032 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 Guilford Neurologic - Moses H Cone Health System Greensboro, North Carolina, United States, 27405 United States, Ohio Cleveland Clinic Hospitals Cleveland, Ohio, United States, 44195 The Ohio State University Columbus, Ohio, United States, 43210 United States, Pennsylvania Thomas Jefferson University Stroke Research Philadelphia, Pennsylvania, United States, 19107 United States, South Carolina Medical University of South Carolina Charleston, South Carolina, United States, 29425 United States, Texas The University Health Science Center at S.A. San Antonio, Texas, United States, 78229-3900 United States, Utah Intermountain Medical Center Murray, Utah, United States, 84157 Germany Universitätsklinikum Leipzig Liebigstraße 22a, Leipzig, Germany, D-04103 Universitatsklinikum Erlangen Erlangen, Germany, D91054 Universitatsklinikum Heidelberg Heidelberg, Germany, D69120 Collapse <<
NCT02011321	Subarachnoid Hemorrhage ... more >> Cerebral Aneurysm Vasospasm, Intracranial Collapse <<	Phase 2	Unknown	September 2015	United States, Michigan ... more >> Henry Ford hospital Not yet recruiting Detroit, Michigan, United States, 48202 Principal Investigator: Panayiotis Varelas, MD, PhD Collapse <<
NCT01480531	Aorta Aneurysm ... more >> Dissection of Aorta Collapse <<	Not Applicable	Withdrawn(We elected to stop t... more >>his study due to our inability to recruit suitable subjects.) Collapse <<	December 2012	United States, North Carolina ... more >> Duke University Medical Center Durham, North Carolina, United States, 27710 Collapse <<
NCT00952081	Hypertension ... more >>Brain Tumor Epilepsy Collapse <<	Phase 4	Completed	-	United States, New York ... more >> NYU Langone Medical Center, Department of Anesthesiology New York, New York, United States, 10016 Collapse <<
NCT03300479	Nontraumatic Intracerebral Hem... more >>orrhage, Multiple Localized Collapse <<	Phase 4	Recruiting	September 30, 2019	Switzerland ... more >> University Hospital Zurich Recruiting Zurich, Switzerland, 8091 Contact: Emanuela Keller, MD Prof. +41 44 255 56 71 emanuela.keller@usz.ch Collapse <<
NCT00952081	-	-	Completed	-	-

Clevidipine/丁酸氯维地平 Catalog No. CSN12960

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