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[CAS NO. 148849-67-6] Ivabradinehydrochloride

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Catalog:	HY-B0162A
Brand:	MCE
CAS:	148849-67-6

Overview

MDL	MFCD00929899
Molecular Weight	505.05
Molecular Formula	C27H37ClN2O5
SMILES	O=C1N(CCCN(C[C@@H]2C3=CC(OC)=C(OC)C=C3C2)C)CCC4=CC(OC)=C(OC)C=C4C1.Cl

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

[1]J Cell Physiol. 2019 Feb;234(2):1925-1936.
[2]Front Pharmacol. 2021 Jun 22;12:696635.

Summary

Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity ^[1] ^[2] ^[3] ^[4] .

In Vivo

Ivabradine hydrochloride (1, 10, 20 mg/kg; i.p.) shows anticonvulsant and neuroprotective action in mice ^[3] .
Ivabradine hydrochloride (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) lowers heart rate in mice with enhanced sympathoadrenergic activities ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	25-30 g, 6 weeks male Swiss mice ^[3]
Dosage:	1, 10, 20 mg/kg
Administration:	I.p.; for 3 days
Result:	Attenuated PTZ- and PICRO-induced seizures while presented an antioxidant effect in all brain areas studied, and reduced cleaved caspase-3 expression in the CA1 and DG region of PICRO- and PTZ-treated mice, respectively.

Animal Model:	3-4 months transgenic (TG) mice with cardiac-restricted overexpression of b2AR ^[4]
Dosage:	5, 10, 20 mg/kg
Administration:	P.o; daily for 1 weeks
Result:	Reduced the maximal HR increase in response to the b-agonist isoproterenol, without modifying the response of contractile parameters at 10 mg/kg.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03405831	Finn Gustafsson\|Danish Heart Foundation\|Rigshospitalet, Denmark	Cardiac Allograft Vasculopathy\|Transplanted Heart Complication	April 17, 2018	Phase 4
NCT00143507	Institut de Recherches Internationales Servier\|Servier	Coronary Disease\|Ventricular Dysfunction, Left	December 2004	Phase 3
NCT04111133	Postgraduate Institute of Medical Education and Research	Cirrhotic Cardiomyopathy\|Left Ventricular Dysfunction\|Cirrhosis, Liver\|Portal Hypertension	January 1, 2020	Not Applicable
NCT03619187	Amgen	Heart Transplantation, Elevated Resting Heart Rate	November 2, 2018	Phase 3
NCT04405804	Bambino Gesù Hospital and Research Institute\|Ministero della Salute, Italy	Acute Heart Failure\|Dilated Cardiomyopathy	June 20, 2020	Phase 2
NCT02166060	Medical University of Warsaw	Heart Failure	August 2014	Phase 4
NCT04580342	Ahmed talaat ahmed aly\|Assiut University	Hypotension	October 15, 2020	Phase 2
NCT03105219	Nanjing First Hospital, Nanjing Medical University	Diabetic Kidney Disease	July 1, 2017	Phase 3
NCT03168529	Phillip Levy\|Amgen\|iRhythm Technologies, Inc.\|Wayne State University	Heart Failure	July 1, 2018	Phase 4
NCT01768585	University Hospital, Saarland\|Universität des Saarlandes	Coronary Artery Disease\|Coronary Arteriosclerosis	December 2012	Phase 4
NCT04436016	University Hospital, Geneva	Myocardial Injury\|Myocardial Ischemia	October 5, 2020	Phase 4
NCT03182725	University of California, San Diego\|Amgen	Postural Orthostatic Tachycardia Syndrome	February 6, 2018	Phase 3
NCT03830957	Rajaie Cardiovascular Medical and Research Center	Heart Failure\|CT Angiography\|Ischemic Cardiomyopathy\|Non-ischemic Cardiomyopathy\|Heart Failure, Systolic\|Heart Failure?Congestive\|Heart Failure, Diastolic\|Heart Rate Low	November 26, 2018	Not Applicable
NCT03718273	Adolfo Fontenla\|Spanish Clinical Research Networt (SCReN)\|Carlos III Health Institute\|Hospital Universitario 12 de Octubre	Atrial Fibrillation\|Heart Diseases	October 19, 2018	Phase 3
NCT02827500	Duke University\|Amgen	Heart Failure	July 2016	Phase 4
NCT02441218	Institut de Recherches Internationales Servier\|Servier	Chronic Heart Failure	September 2006	Phase 3
NCT03367026	Peking Union Medical College Hospital	Sepsis, Severe	January 1, 2018	Not Applicable
NCT05279651	Jagiellonian University\|Population Health Research Institute\|Vanderbilt University Medical Center	Myocardial Injury After Noncardiac Surgery (MINS)\|Myocardial Ischemia	June 13, 2022	Phase 3
NCT01022463	Govind Ballabh Pant Hospital	Mitral Stenosis	November 2009	Phase 3
NCT02236247	University of Sao Paulo\|Fundação de Amparo à Pesquisa do Estado de São Paulo	Decompensated Heart Failure	May 2013	Phase 1\|Phase 2
NCT02294292	Institute of Liver and Biliary Sciences, India	Diastolic Dysfunction\|Chronic Liver Disease	July 1, 2014	Not Applicable
NCT04031573	Assistance Publique - Hôpitaux de Paris	Septic Shock	February 24, 2021	Phase 3
NCT04030546	Vilnius University	Patients With Cancer	June 1, 2019	Phase 3
NCT03387605	Loyola University\|Amgen	Heart Failure\|Cardiogenic Shock\|Tachycardia	March 15, 2018	Phase 4
NCT02623569	Xintong Pharmacy Company	Angina Pectoris	October 2014	Phase 2
NCT02086422	The Leeds Teaching Hospitals NHS Trust	Chronic Heart Failure	July 2013	Not Applicable
NCT00202579	Institut de Recherches Internationales Servier\|Servier	Heart Failure, Congestive	September 2004	Phase 2
NCT04448899	Damanhour University	Congestive Heart Failure	June 1, 2020	Phase 4
NCT01365286	Medical University of Lodz	Asthma, Chronic Obstructive Pulmonary Disease (COPD)	May 2009	Phase 4
NCT01178528	IRCCS San Raffaele	Heart Failure	September 2009	Phase 3
NCT01186783	Martin-Luther-Universität Halle-Wittenberg\|Servier\|KKS Netzwerk	Multiple Organ Dysfunction Syndrome	May 2010	Phase 2
NCT04853797	Danish Headache Center	Headache, Migraine	April 16, 2021	Not Applicable
NCT01699776	Cocco, Giuseppe, M.D.\|Cardiology Office, Rheinfelden, Switzerland	Cardiac Failure	April 2008	Phase 4
NCT00202566	Institut de Recherches Internationales Servier\|Servier	Angina Pectoris	June 2005	Phase 3
NCT03456856	Amgen	Heart Failure (HF)	September 28, 2017	Phase 4
NCT04308031	Chun-Yao Huang\|Taipei Medical University Hospital	Atrial Fibrillation\|Ivabradine\|Heart Failure	August 26, 2018	Phase 3
NCT01761825	Tel-Aviv Sourasky Medical Center	Postural Tachycardia Syndrome	December 2012	Phase 2
NCT02188082	Jiangsu HengRui Medicine Co., Ltd.	Chronic Systolic Heart Failure	May 2014	Phase 2\|Phase 3
NCT02446990	Institut de Recherches Internationales Servier\|Servier	Coronary Artery Disease	September 2009	Phase 3
NCT03710057	Getz Pharma	Chronic Heart Failure	December 1, 2016
NCT00865917	Hannover Medical School\|Charite University, Berlin, Germany	Postural Orthostatic Tachycardia Syndrome	November 2008	Phase 2
NCT01425164	University of Campania Luigi Vanvitelli\|IRCCS San Raffaele	Coronary Heart Disease\|Angina\|Hemodialysis	January 2011	Phase 4
NCT03987204	Yale University	Atrial Fibrillation\|Atrial Fibrillation, Persistent	June 15, 2019	Phase 1
NCT04208594	Alexandria University	Ivabradine\|Propranolol\|Hypotensive Anesthesia	December 11, 2019	Not Applicable
NCT01868880	Policlinico Casilino ASL RMB	Heart Rate Control in ICD Patients With Heart Failure	February 2016	Phase 4
NCT03437369	Hospital Universitario Ramon y Cajal	Cardiogenic Shock	May 2018	Phase 4
NCT05261464	Mahidol University	Heart Rate\|Coronary Computed Tomography Angiography	January 30, 2021	Phase 4
NCT03701880	Ain Shams University\|Sadat City University	Heart Failure With Reduced Ejection Fraction\|Decompensated Heart Failure	September 16, 2018	Not Applicable
NCT05168189	Assiut University	AF - Atrial Fibrillation	August 2022
NCT00815100	Hospital Universitario de Canarias	Acute Coronary Syndromes	April 2009	Phase 4
NCT02764970	Medical University of Graz	Bradycardia	February 2015
NCT01039389	University Hospital Inselspital, Berne	Coronary Artery Disease	October 2009	Not Applicable
NCT02681978	Campus Bio-Medico University	Coronary Artery Disease	February 2014	Phase 4
NCT02584439	University Hospital, Rouen\|Institut National de la Santé Et de la Recherche Médicale, France	Healthy\|Vascular Stiffness\|Aging	October 2015	Phase 3
NCT01657136	Policlinico Casilino ASL RMB	Inappropriate Sinus Tachycardia	September 2013	Phase 3
NCT02354573	University of Oxford\|University of Aberdeen	Heart Failure	December 2011	Not Applicable
NCT05348057	Qian geng\|Chinese PLA General Hospital	Cardiovascular Diseases	August 1, 2021	Phase 4
NCT00825123	Bayside Health\|Baker Heart and Diabetes Institute	Central Arterial Pressure	October 2008	Phase 4
NCT03866395	Azienda Policlinico Umberto I	Angina Pectoris, Stable	March 5, 2015	Phase 4
NCT01796093	Cocco, Giuseppe, M.D.\|Cardiology Office, Rheinfelden, Switzerland	Heart Failure\|Atrial Fibrillation	April 2008
NCT05594342	The Young Investigator Group of Cardiovascular Research	Heart Failure\|Cardiogenic Shock\|Ischemic Heart Disease	July 1, 2022	Phase 3
NCT04285736	Cairo University\|National Heart Institute, Egypt	NSTEMI	December 2014	Phase 2\|Phase 3
NCT01804010	Asan Medical Center\|Institut de Recherches Internationales Servier	Healthy Individual	May 2007	Phase 1
NCT03137537	Dana-Farber Cancer Institute\|Amgen	Lymphoma\|Autonomic Imbalance\|Cancer Survivorship	February 27, 2018	Phase 2
NCT05481177	Uniformed Services University of the Health Sciences	Long Haul COVID\|Postural Orthostatic Tachycardia Syndrome	November 15, 2022	Phase 4
NCT02973594	University of Colorado, Denver\|American Heart Association\|Ohio State University	Dilated Cardiomyopathies, Idiopathic\|Heart Failure, Systolic\|Ventricular Remodeling\|Electrical Remodeling	November 2016	Phase 4
NCT01755663	Col. Suthee Panichkul\|Phramongkutklao College of Medicine and Hospital	Coronary Artery Disease	December 2014	Phase 4
NCT03245996	Tartu University Hospital	Aortic Blood Pressure	June 2015	Phase 4
NCT05141071	Cairo University	Septic Shock	November 25, 2021	Phase 2
NCT02247245	University of Leeds	Chronic Heart Failure\|Atrial Fibrillation\|Arrhythmia, Sinus	September 2014	Not Applicable
NCT01364077	University of Campania Luigi Vanvitelli	High Heart Rate	January 2010	Phase 4
NCT01373619	University of Campania Luigi Vanvitelli	Heart Failure	January 2010	Phase 4
NCT03485482	Ain Shams University	Cardiovascular Diseases	March 1, 2018	Phase 3
NCT04186286	University of Calgary\|Dysautonomia International	Postural Tachycardia Syndrome	February 1, 2021	Phase 2
NCT02507050	Liverpool Heart and Chest Hospital NHS Foundation Trust	Coronary Artery Disease\|Angina	March 2016	Phase 4
NCT02046044	Kocaeli University	Heart Failure	January 2014	Phase 4
NCT03650205	University of Sao Paulo	Neoplasms\|Heart Failure\|Cardiotoxicity\|Chemotherapy Effect\|Oncology	January 22, 2019	Not Applicable
NCT01029223	Bayside Health	Blood Pressure	October 2008	Phase 4
NCT00757055	St Vincent´s University Hospital, Ireland	Diastolic Heart Failure	December 2012	Phase 2
NCT03631654	University of Maryland, Baltimore\|Stanford University	Heart Failure NYHA Class IV	October 1, 2020	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 50 mg/mL ( 99.00 mM ; Need ultrasonic)

DMSO : 25 mg/mL ( 49.50 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9800 mL	9.9000 mL	19.8000 mL
5 mM	0.3960 mL	1.9800 mL	3.9600 mL
10 mM	0.1980 mL	0.9900 mL	1.9800 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 50 mg/mL (99.00 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Tardif JC, et al. Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable angina. Eur Heart J. 2005 Dec;26(23):2529-36.
[2] Mulder P, et al. Heart rate slowing for myocardial dysfunction/heart failure. Adv Cardiol. 2006;43:97-105.
[3] Cavalcante TMB, et al. Ivabradine possesses anticonvulsant and neuroprotective action in mice. Biomed Pharmacother. 2019 Jan;109:2499-2512.
[4] Du XJ, et al. I(f) channel inhibitor ivabradine lowers heart rate in mice with enhanced sympathoadrenergic activities. Br J Pharmacol. 2004 May;142(1):107-12.

Synonyms

2H-3-Benzazepin-2-one, 3-[3-[[[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-, hydrochloride (1:1)

2H-3-Benzazepin-2-one, 3-[3-[[(3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl)methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-, monohydrochloride, (S)-

2H-3-Benzazepin-2-one, 3-[3-[[[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-, monohydrochloride

Bicyclo[4.2.0]octane, 2H-3-benzazepin-2-one deriv.

Ivabradine hydrochloride

Corlentor

Procoralan

Corlanor

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