Ivabradine
Based on 4 publication(s) in Google Scholar
Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity.
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- Purity : 99.94%
- CAS No.: 155974-00-8
- 화학식: C27H36N2O5
- 분자량:468.59
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ivabradine
More
Customer Validation & Images
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WB
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
4.28 μM
Compound: Ivabradine
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Blockade of human HCN4 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay
Blockade of human HCN4 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay
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[PMID: 20795648] |
| HEK293 | EC50 |
4.5 μM
Compound: Ivabradine
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Blockade of mouse HCN1 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay
Blockade of mouse HCN1 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay
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[PMID: 20795648] |
| HEK293 | EC50 |
4.52 μM
Compound: Ivabradine
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Blockade of mouse HCN2 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay
Blockade of mouse HCN2 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay
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[PMID: 20795648] |
In Vivo
Ivabradine (5, 10, 20 mg/kg;p.o.; daily for 1 weeks) lowers heart rate in mice with enhanced sympathoadrenergic activities[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:25-30 g, 6 weeks male Swiss mice[3]
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Dosage:1, 10, 20 mg/kg
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Administration:I.p.; for 3 days
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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.
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Animal Model:3-4 months transgenic (TG) mice with cardiac-restricted overexpression of b2AR[4]
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Dosage:5, 10, 20 mg/kg
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Administration:P.o; daily for 1 weeks
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Result:Reduced the maximal HR increase in response to the b-agonist isoproterenol, without modifying the response of contractile parameters at 10 mg/kg.
Chemical Information
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CAS No. 155974-00-8
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Appearance Solid
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분자량 468.59
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화학식 C27H36N2O5
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Color White to light yellow
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SMILES
O=C1N(CCCN(C[C@@H]2C3=CC(OC)=C(OC)C=C3C2)C)CCC4=CC(OC)=C(OC)C=C4C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (4)
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Journal Impact Factor
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Most Recent
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Front Pharmacol
Ivabradine Ameliorates Cardiac Diastolic Dysfunction in Diabetic Mice Independent of Heart Rate Reduction. [Abstract]2021 Jun 22:12:696635. PMID: 34239443
Ivabradine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Jun 22:12:696635. [Abstract]
NRCFs were pretreated with or without Ivabradine (10-40 μM) at the indicated concentrations for 30 min, and then exposed to HG for 48 h. JNK and p38 MAPK phosphorylation and total JNK and p38 MAPK expression were determined by western blotting.
Ivabradine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Jun 22:12:696635. [Abstract]
NRCFs were treated with or without ivabradine at the indicated concentrations for 30 min, and then exposed to HG for 48 h. The protein expression of PCNA, α-SMA, TIMP2, collagen I, collagen III, and MMP2 was determined by western blotting.
Ivabradine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Jun 22:12:696635. [Abstract]
NRCFs were treated with or without ivabradine at the indicated concentrations for 30 min, and then exposed to HG for 48 h. The cell proliferation rate was determined using an MTT assay.
Ivabradine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Jun 22:12:696635. [Abstract]
Effects of ivabradine and zatebradine on heart rate (HR) and biometric parameters. During treatment with or without Ivabradine (20 mg/kg) for 7–11 weeks, the mean HR of mice was recorded by electrocardiography (ECG).
Ivabradine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Jun 22:12:696635. [Abstract]
Mice were treated with or without Ivabradine (20 mg/kg) for 7–11 weeks, and their blood glucose concentration was measured.
Ivabradine purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2021 Jun 22:12:696635. [Abstract]
Mice were treated with or without Ivabradine (20 mg/kg) for 7–11 weeks, and their body mass was measured.
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J Cell Physiol
Inhibition of JNK and p38 MAPK-mediated inflammation and apoptosis by ivabradine improves cardiac function in streptozotocin-induced diabetic cardiomyopathy. [Abstract]2019 Feb;234(2):1925-1936. PMID: 30067872
Ivabradine purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Feb;234(2):1925-1936. [Abstract]
Protein expression levels of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, and IL-6 are detected by western blotting.
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Mol Biol Rep
Cardiac drug potential: exploring individual and combined cardiac drugs to promote differentiation of adipose-derived stem cells into cardiomyocytes. [Abstract]2026 Feb 26;53(1):434. PMID: 41746444 -
용액&용해도
In Vitro:
DMSO : 100 mg/mL (213.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. Mulder P, et al. Heart rate slowing for myocardial dysfunction/heart failure. Adv Cardiol. 2006;43:97-105. [Content Brief]
[3]. Cavalcante TMB, et al. Ivabradine possesses anticonvulsant and neuroprotective action in mice. Biomed Pharmacother. 2019 Jan;109:2499-2512. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1341 mL | 10.6703 mL | 21.3406 mL | 53.3515 mL |
| 5 mM | 0.4268 mL | 2.1341 mL | 4.2681 mL | 10.6703 mL | |
| 10 mM | 0.2134 mL | 1.0670 mL | 2.1341 mL | 5.3352 mL | |
| 15 mM | 0.1423 mL | 0.7114 mL | 1.4227 mL | 3.5568 mL | |
| 20 mM | 0.1067 mL | 0.5335 mL | 1.0670 mL | 2.6676 mL | |
| 25 mM | 0.0854 mL | 0.4268 mL | 0.8536 mL | 2.1341 mL | |
| 30 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7784 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 50 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0670 mL | |
| 60 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL | |
| 80 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6669 mL | |
| 100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5335 mL |
Ivabradine Related Classifications
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