Ivabradine HCl (Procoralan)

Alias: S 16257-2;Corlanor; S-16257-2; Coraxan; Ivabid;S16257-2; Ivabradine HCl; Corlentor; Procoralan; Coralan; Bradia
Cat No.:V1142 Purity: ≥98%
Ivabradine HCl (Corlentor; Corlanor; Coraxan; Ivabid; Procoralan; Coralan; S16257; S 16257; S-16257; Bradia), the hydrochloride salt of Ivabradine, is a novel and potent cardiac pacemaker current (If) inhibitor with antianginal effects.
Ivabradine HCl (Procoralan) Chemical Structure CAS No.: 148849-67-6
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
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Other Forms of Ivabradine HCl (Procoralan):

  • Ivabradine metabolite N-Demethyl Ivabradine hydrochloride
  • Ivabradine-d6 hydrochloride
  • Ivabradine
  • Ivabradine D3 HCl
  • Ivabradine sulfate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ivabradine HCl (Corlentor; Corlanor; Coraxan; Ivabid; Procoralan; Coralan; S16257; S 16257; S-16257; Bradia), the hydrochloride salt of Ivabradine, is a novel and potent cardiac pacemaker current (If) inhibitor with antianginal effects. It suppresses IF with IC50 of 2.9 μM. Ivabradine is a pure heart rate reducer that works exclusively on the sinoatrial node's pacemaker activity. A novel medication called ivabradine is prescribed to treat stable angina pectoris symptomatically. In contrast to beta blockers and calcium channel blockers, two frequently prescribed antianginal medications, ivabradine works by selectively inhibiting the funny channel to lower heart rate.

Biological Activity I Assay Protocols (From Reference)
Targets
Adrenergic Receptor
ln Vitro

In vitro activity: Ivabradine HCl (also referred to as S 16257-2), a new If inhibitor with an IC 50 of 2.9 μM that selectively inhibits the sinoatrial node's pacemaker activity, is a pure heart rate reducer. A novel medication called ivabradine is used to treat stable angina pectoris symptomatically. Ivabradine works by selectively inhibiting the funny channel to lower heart rate; this is not the same mechanism as beta blockers or calcium channel blockers, two commonly prescribed antianginal medications.

ln Vivo
Ivabradine hydrochloride (1, 10, 20 mg/kg; i.p.) exhibits anticonvulsant and neuroprotective properties in mice[3]. Ivabradine hydrochloride (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) reduces heart rate in mice with increased sympathoadrenergic activity[4].
Animal Protocol
25-30 g, 6 weeks male Swiss mice
1, 10, 20 mg/kg
I.p.; for 3 days
References

[1]. 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]. Heart rate slowing for myocardial dysfunction/heart failure. Adv Cardiol. 2006;43:97-105.

[3]. Ivabradine possesses anticonvulsant and neuroprotective action in mice. Biomed Pharmacother. 2019 Jan;109:2499-2512.

[4]. I(f) channel inhibitor ivabradine lowers heart rate in mice with enhanced sympathoadrenergic activities. Br J Pharmacol. 2004 May;142(1):107-12.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H37CLN2O5
Molecular Weight
505.05
Exact Mass
504.24
Elemental Analysis
C, 64.21; H, 7.38; Cl, 7.02; N, 5.55; O, 15.84
CAS #
148849-67-6
Appearance
Solid powder
SMILES
CN(CCCN1CCC2=CC(=C(C=C2CC1=O)OC)OC)C[C@H]3CC4=CC(=C(C=C34)OC)OC.Cl
InChi Key
HLUKNZUABFFNQS-ZMBIFBSDSA-N
InChi Code
InChI=1S/C27H36N2O5.ClH/c1-28(17-21-11-20-14-25(33-4)26(34-5)16-22(20)21)8-6-9-29-10-7-18-12-23(31-2)24(32-3)13-19(18)15-27(29)30;/h12-14,16,21H,6-11,15,17H2,1-5H3;1H/t21-;/m1./s1
Chemical Name
3-[3-[[(7S)-3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one;hydrochloride
Synonyms
S 16257-2;Corlanor; S-16257-2; Coraxan; Ivabid;S16257-2; Ivabradine HCl; Corlentor; Procoralan; Coralan; Bradia
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 25~101 mg/mL (49.5~200 mM)
Water: ~82 mg/mL (~162.4 mM)
Ethanol: ~101 mg/mL (~200 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05973591 Active
Recruiting
N/A Dilated Cardiomyopathy
Ventricular Remodeling
Yonsei University July 15, 2023 N/A
NCT05882708 Recruiting Drug: Ivabradine Sepsis
Ivabradine
Hemodynamics
Second Affiliated Hospital of
Guangzhou Medical University
June 1, 2023 Phase 4
NCT03168529 Recruiting Drug: Placebo
Drug: Ivabradine
Heart Failure Phillip Levy July 1, 2018 Phase 4
NCT05348057 Recruiting Drug: Ivabradine Cardiovascular Diseases Qian geng August 1, 2021 Phase 4
NCT05481177 Recruiting Drug: Ivabradine Long Haul COVID
Postural Orthostatic Tachycardia
Syndrome
Uniformed Services University
of the Health Sciences
June 14, 2023 Phase 4
Biological Data
  • Ivabradine HClIvabradine administration attenuates post‐MI LV remodeling.J Am Heart Assoc. 2016 Apr; 5(4): e002989.
  • Ivabradine HCl
    Ivabradine administration reduces the extent of wall thinning after MI.J Am Heart Assoc. 2016 Apr; 5(4): e002989.
  • Ivabradine HCl
    Ivabradine administration reduces post‐MI LV dyssynchrony.J Am Heart Assoc. 2016 Apr; 5(4): e002989.
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