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Ivabradine hydrochloride

Ivabradine hydrochloride structure

CAS No:
148849-67-6
Formula:
C27H36N2O5.ClH
Chemical Name:
Ivabradine hydrochloride
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
Categories:
Biochemical Engineering > Inhibitors

Description

Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.

Ivabradine hydrochloride is a hydrochloride obtained by combining ivabradine with one molar equivalent of hydrochloric acid. Used to treat patients with angina who have intolerance to beta blockers and/or heart failure. It has a role as a cardiotonic drug. It contains an ivabradine(1+).|Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization. This decreases heart rate, reduces myocardial oxygen demand and allows more time for blood to flow to the myocardium without affecting cardiac contractility. HCN channels, mixed sodium (Na+) and potassium (K+) channels that carry the inward If current, play a key role in the regulation of pacemaker firing rate in the SA node. The If pacemaker current, the inward flow of positively charged Na+-K+ ions, initiates the spontaneous diastolic depolarization phase and modulating heart rate.|A benzazepine derivative and selective HYPERPOLARIZATION-ACTIVATED CYCLIC NUCLEOTIDE-GATED CHANNELS inhibitor that lowers the heart rate. It is used in the treatment of CHRONIC STABLE ANGINA in patients unable to take BETA-ADRENERGIC BLOCKERS, and in the treatment of HEART FAILURE.

Ivabradine hydrochloride Basic Attributes

Molecular Weight：

505.05

Exact Mass：

504.239105

EC Number：

1308068-626-2

UNII：

TP19837BZK

DSSTox ID：

DTXSID2046913

NCI Thesaurus Code：

C148546

ATC Code：

C01EB17

Characteristics

PSA：

60.5

XLogP3：

4.04990

Appearance：

white to beige

Melting Point：

193-196°C

Boiling Point：

626.9°C at 760 mmHg

Flash Point：

332.9ºC

Water Solubility：

H2O: ≥5mg/mL (warmed)

Storage Conditions：

-20°C Freezer

Vapor Pressure：

1.24E-15mmHg at 25°C

Specific rotation：

58921 +7.8°; 36521 +27.8° (c = 1% in DMSO)

Safety Information

Transport codes：

UN 3077 9 / PGIII

hazard class code：

50/53

safety instructions：

60-61

Marks：

Precautionary statement(s)：

P273

Hazard Statements：

H400

GHS Classification：

|Danger|H302 (10.64%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P264, P270, P273, P281, P301+P312, P308+P313, P314, P330, P391, P405, and P501|Aggregated GHS information provided by 47 companies from 8 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Symptomatic treatment of chronic stable angina pectoris Ivabradine is indicated for the symptomatic treatment of chronic stable angina pectoris in coronary artery disease adults with normal sinus rhythm and heart rate ≥ 70 bpm. Ivabradine is indicated:in adults unable to tolerate or with a contra-indication to the use of beta-blockersorin combination with beta-blockers in patients inadequately controlled with an optimal beta-blocker dose. Treatment of chronic heart failure Ivabradine is indicated in chronic heart failure NYHA II to IV class with systolic dysfunction, in patients in sinus rhythm and whose heart rate is ≥ 75 bpm, in combination with standard therapy including beta-blocker therapy or when beta-blocker therapy is contraindicated or not tolerated.|Symptomatic treatment of chronic stable angina pectorisIvabradine is indicated for the symptomatic treatment of chronic stable angina pectoris in coronary artery disease adults with normal sinus rhythm and heart rate ≥ 70 bpm. Ivabradine is indicated:in adults unable to tolerate or with a contraindication to the use of beta-blockersor in combination with beta-blockers in patients inadequately controlled with an optimal beta-blocker dose.Treatment of chronic heart failureIvabradine is indicated in chronic heart failure NYHA II to IV class with systolic dysfunction, in patients in sinus rhythm and whose heart rate is ≥ 75 bpm, in combination with standard therapy including beta-blocker therapy or when beta-blocker therapy is contraindicated or not tolerated.|Symptomatic treatment of chronic stable angina pectoris Ivabradine is indicated for the symptomatic treatment of chronic stable angina pectoris in coronary artery disease adults with normal sinus rhythm and heart rate ≥ 70 bpm. Ivabradine is indicated :in adults unable to tolerate or with a contraindication to the use of beta-blockersor in combination with beta-blockers in patients inadequately controlled with an optimal beta-blocker dose.Treatment of chronic heart failure Ivabradine is indicated in chronic heart failure NYHA II to IV class with systolic dysfunction, in patients in sinus rhythm and whose heart rate is ≥ 75 bpm, in combination with standard therapy including beta-blocker therapy or when beta-blocker therapy is contraindicated or not tolerated.|Symptomatic treatment of chronic stable angina pectoris, , Ivabradine is indicated for the symptomatic treatment of chronic stable angina pectoris in coronary artery disease adults with normal sinus rhythm and heart rate ≥ 70 bpm., , Ivabradine is indicated :, , - in adults unable to tolerate or with a contra-indication to the use of beta-blockers, , - or in combination with beta-blockers in patients inadequately controlled with an optimal beta-blocker dose., , Treatment of chronic heart failure, , Ivabradine is indicated in chronic heart failure NYHA II to IV class with systolic dysfunction, in patients in sinus rhythm and whose heart rate is ≥ 75 bpm, in combination with standard therapy including beta-blocker therapy or when beta-blocker therapy is contraindicated or not tolerated. (see section 5.1),|Symptomatic treatment of chronic stable angina pectoris in coronary artery disease adults with normal sinus rhythm and heart rate ≥ 70 bpm. Ivabradine is indicated: - in adults unable to tolerate or with a contra-indication to the use of beta-blockers - or in combination with beta-blockers in patients inadequately controlled with an optimal beta-blocker dose. Treatment of chronic heart failure Ivabradine is indicated in chronic heart failure NYHA II to IV class with systolic dysfunction, in patients in sinus rhythm and whose heart rate is ≥ 75 bpm, in combination with standard therapy including beta-blocker therapy or when beta-blocker therapy is contraindicated or not tolerated.,|Treatment of heart failure, Treatment of ischaemic coronary artery disorders|Treatment of ischaemic coronary artery disorders|Treatment of angina pectoris, Treatment of chronic heart failure, Treatment of coronary artery disease

MeSH：

Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume. (See all compounds classified as Cardiovascular Agents.)

MeSH Entry Terms：

7,8-dimethoxy-3-(3-(((4,5-dimethoxybenzocyclobutan-1-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-2H-benzazepin-2-one

Ivabradine hydrochloride Use and Manufacturing

Uses

Selective bradycardic agent with direct effect on the pacemaker If current of the sinoatrial node. Antianginal

Use Classification：

Human drugs -> Ivabradine Zentiva -> EMA Drug Category|Cardiac therapy -> Human pharmacotherapeutic group|Human drugs -> Corlentor -> EMA Drug Category|Human drugs -> Procoralan -> EMA Drug Category|Human drugs -> Ivabradine Accord -> EMA Drug Category|Human drugs -> Ivabradine JensonR -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:505.0
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:10
Exact Mass:504.2391000
Monoisotopic Mass:504.2391000
Topological Polar Surface Area:60.5
Heavy Atom Count:35
Complexity:663
Defined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

No detailed description provided

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

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Registered Holders

MAITHRI LABORATORIES PRIVATE LTD

United States
Active
ALEMBIC PHARMACEUTICALS LTD

United States
Active
ZYDUS LIFESCIENCES LTD

United States
Active

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