| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Not applicable for the deuterated internal standard. Unlabeled ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that specifically inhibits the cardiac pacemaker current (If). It acts as an open-channel blocker, gaining access to its binding site only when channels are in the open state.
|
|---|---|
| ln Vitro |
Ivabradine-d6 is not used for measuring intrinsic biological activity; its role is analytical. Unlabeled ivabradine blocks HCN4 and HCN1 channels with half-block concentrations of approximately 2.0 microM and 1.9 microM, respectively. It acts as an open-channel blocker, with binding occurring only when channels are in the open state. It also inhibits hERG potassium channels with similar potency.
|
| ln Vivo |
Ivabradine-d6 itself is not used for in vivo activity studies. Unlabeled ivabradine hydrochloride is used in clinical medicine as a pure heart rate-lowering agent for stable angina pectoris and heart failure. It reduces heart rate in a dose-dependent manner without affecting blood pressure or myocardial contractility. Ivabradine has also demonstrated anticonvulsant activity in preclinical models.
|
| Enzyme Assay |
Ivabradine-d6 is not used in non-cellular binding assays as a test compound. For HCN channel studies, a standard patch-clamp electrophysiology protocol is used. HEK-293 cells expressing HCN4 or HCN1 channels are voltage-clamped, and ivabradine is perfused at varying concentrations. The reduction in hyperpolarization-activated current is measured, and IC50 values are calculated by fitting the Hill equation to the dose-response data.
|
| Cell Assay |
Ivabradine-d6 is not used for cellular assays. For functional studies, rat engineered heart tissue (EHT) or embryoid bodies are used. Ivabradine hydrochloride is added to the culture medium at varying concentrations, and the spontaneous beating rate is measured over time. A reduction in beat rate without changes in contractile force confirms the HCN channel-blocking mechanism in a functional cardiac tissue model.
|
| Animal Protocol |
No in vivo protocol is applicable for Ivabradine-d6 as an internal standard. For pharmacokinetic studies, unlabeled ivabradine is administered orally or intravenously to rats or human subjects. Plasma samples are collected at multiple time points, and a constant amount of Ivabradine-d6 hydrochloride is spiked into each sample as an internal standard. Following protein precipitation, samples are analyzed by LC-MS/MS to quantify unlabeled drug concentrations.
|
| ADME/Pharmacokinetics |
Ivabradine-d6 hydrochloride is chemically identical to the unlabeled analyte except for a +6 Da mass shift due to six deuterium atoms, resulting in virtually identical extraction recovery, chromatographic retention time, and ionization efficiency. It is stable under typical LC-MS conditions and is designed for use as an internal standard in quantitative bioanalysis.
|
| Toxicity/Toxicokinetics |
No direct toxicological data is provided for Ivabradine-d6 hydrochloride, as it is used at trace analytical levels. Unlabeled ivabradine has a well-characterized clinical safety profile; common adverse effects include visual disturbances (phosphenes, luminous phenomena), bradycardia, and atrial fibrillation. The deuterated standard poses negligible toxicity risk when used as intended in analytical assays.
|
| Additional Infomation |
Ivabradine-d6 hydrochloride is a critical bioanalytical tool for pharmacokinetic studies and therapeutic drug monitoring. Unlabeled ivabradine (Procoralan, Corlanor) is a clinically approved drug developed by Servier for the treatment of chronic heart failure and stable angina. The deuterated internal standard enables accurate and precise quantification of ivabradine in biological matrices, supporting regulatory-compliant bioanalytical method validation.
|
| Molecular Formula |
C27H37CLN2O5
|
|---|---|
| Molecular Weight |
505.046087026596
|
| Exact Mass |
510.276
|
| CAS # |
2070009-63-9
|
| Related CAS # |
Ivabradine metabolite N-Demethyl Ivabradine hydrochloride;1246638-08-3;N-Demethyl Ivabradine-d6 hydrochloride;Ivabradine hydrochloride;148849-67-6;Ivabradine;155974-00-8;Ivabradine-d3 hydrochloride;1217809-61-4;Ivabradine-d6
|
| PubChem CID |
92044426
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
35
|
| Complexity |
663
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C([C@H]1CC2=CC(OC)=C(OC)C=C12)N(C)CCCN1CCC2=CC(OC([H])([H])[H])=C(OC([H])([H])[H])C=C2CC1=O.Cl
|
| InChi Key |
HLUKNZUABFFNQS-SNBVEVFOSA-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/i2D3,3D3;
|
| Chemical Name |
3-[3-[[(7S)-3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-bis(trideuteriomethoxy)-2,5-dihydro-1H-3-benzazepin-4-one;hydrochloride
|
| 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 (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
|
|---|---|
| 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
