| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The hyperpolarization-activated cyclic nucleotide-gated (HCN) channel, specifically the HCN4 channel responsible for the pacemaker current (If) in the sinoatrial node. Ivabradine D3 HCl is a selective and specific inhibitor of the If current, reducing the slope of the diastolic depolarization phase of the cardiac action potential, which leads to a reduction in heart rate without affecting other cardiac electrophysiological properties.
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| ln Vitro |
As a deuterium-labeled internal standard, Ivabradine D3 HCl is chemically identical to the active pharmaceutical ingredient Ivabradine HCl, with the exception of the isotopic substitution. Its pharmacological activity is expected to be the same as Ivabradine, which is a selective inhibitor of the cardiac pacemaker current (If). It reduces heart rate by acting on the sinoatrial node.
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| ln Vivo |
The in vivo activity of Ivabradine D3 HCl is expected to be the same as Ivabradine hydrochloride. Ivabradine is clinically used to reduce heart rate in patients with chronic stable angina and heart failure. It selectively inhibits the If current in the sinoatrial node, resulting in a dose-dependent reduction in heart rate.
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| Enzyme Assay |
Ivabradine D3 HCl is not typically used in in vitro pharmacological assays as a test compound. Instead, it is used as an internal standard in analytical methods. However, the non-labeled Ivabradine is studied in vitro using patch-clamp techniques on isolated sinoatrial node cells or on cells expressing HCN channels to measure its inhibition of the If current.
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| Cell Assay |
Ivabradine D3 HCl is not typically used in cell-based assays as a test compound. Its primary application is as an internal standard in LC-MS/MS methods for the quantification of Ivabradine in biological samples. Cell-based assays for the non-labeled Ivabradine would involve measuring its effect on the firing rate of sinoatrial node cells or on HCN channel-expressing cells.
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| Animal Protocol |
Ivabradine D3 HCl is not used in animal studies as a test compound. It is used as an internal standard in pharmacokinetic studies to quantify Ivabradine levels in plasma and tissues from animals dosed with Ivabradine. The pharmacokinetic profile of Ivabradine has been studied in various animal models.
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| ADME/Pharmacokinetics |
Ivabradine D3 HCl has a molecular weight that is 3 Da higher than Ivabradine HCl due to the deuterium substitution. This mass difference allows for its use as an internal standard in mass spectrometry. As a labeled compound, its physicochemical properties, such as solubility and stability, are similar to Ivabradine HCl. It should be stored as powder at -20°C.
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| Toxicity/Toxicokinetics |
No specific toxicity data are documented for Ivabradine D3 HCl. As a deuterium-labeled compound used as an internal standard, it is typically handled in very small quantities. The safety profile of Ivabradine HCl is well-established from its clinical use. It is contraindicated in patients with severe hypotension, cardiogenic shock, and certain cardiac arrhythmias.
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| Additional Infomation |
Ivabradine D3 HCl is a stable isotope-labeled internal standard used in LC-MS/MS methods for the quantification of Ivabradine in pharmacokinetic, bioequivalence, and therapeutic drug monitoring studies. The deuterium labeling provides a mass shift that allows for the differentiation of the internal standard from the analyte. It is intended for research use only.
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| Molecular Formula |
C27H34D3CLN2O5
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|---|---|
| Molecular Weight |
505.04608
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| Exact Mass |
507.26
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| CAS # |
1217809-61-4
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| Related CAS # |
Ivabradine metabolite N-Demethyl Ivabradine hydrochloride; 1246638-08-3; N-Demethyl Ivabradine-d6 hydrochloride; Ivabradine hydrochloride; 148849-67-6; Ivabradine-d6 hydrochloride; 2070009-63-9; Ivabradine; 155974-00-8; Ivabradine-d6
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| PubChem CID |
46782006
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.049
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
663
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[H]Cl.COC1=C(OC)C=C(CCN(CCCN(C([2H])([2H])[2H])C[C@@H]2C(C=C(OC)C(OC)=C3)=C3C2)C(C4)=O)C4=C1
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| InChi Key |
HLUKNZUABFFNQS-AFMQDYKRSA-N
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| 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/i1D3
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| Chemical Name |
3-[3-[[(7S)-3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-(trideuteriomethyl)amino]propyl]-7,8-dimethoxy-2,5-dihydro-1H-3-benzazepin-4-one;hydrochloride
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| Synonyms |
Ivabradine-d3 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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