| Size | Price | Stock | Qty |
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| 1mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Lidoflazine targets multiple ion channels and receptors. Its primary therapeutic target is the L-type calcium channel, where it acts as a non-selective calcium channel blocker to produce coronary vasodilation. However, it binds with high affinity to the hERG potassium channel (IC50 < 0.1 μM, approximately 16 nM), which is responsible for the rapid delayed rectifier potassium current (IKr) in cardiac myocytes. This off-target interaction is the primary cause of its cardiotoxicity. Lidoflazine is also reported to have some antiarrhythmic actions.
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| ln Vitro |
When HEK 293 cells stably express wild-type HERG, lidoflazine potently inhibits HERG currents (IHERG) (IC50 around 16 nM).
In vitro, Lidoflazine potently inhibits the hERG potassium current (IHERG) recorded from HEK 293 cells stably expressing the wild-type hERG channel, with an IC50 of approximately 16 nM. This high-affinity blockade of the hERG channel underlies the compound's significant risk of QT interval prolongation. As a calcium channel blocker, it inhibits calcium influx through voltage-gated calcium channels, leading to vasodilation of coronary and peripheral arteries. The compound's in vitro activity against calcium channels is well-documented, though specific IC50 values for calcium channel blockade are less prominently reported than its hERG activity. |
| ln Vivo |
In vivo, Lidoflazine demonstrates antianginal efficacy through its calcium channel-blocking activity, which reduces cardiac workload and improves coronary blood flow. However, its clinical utility is overshadowed by its potent hERG-blocking activity, which causes dose-dependent prolongation of the QT interval on the electrocardiogram. This prolongation creates a significant risk of torsade de pointes, a potentially fatal ventricular arrhythmia. In animal models and human subjects, the drug's cardiovascular effects are closely monitored due to this arrhythmogenic potential.
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| Enzyme Assay |
In vitro hERG channel binding/functional assays are the primary method for assessing Lidoflazine's receptor interaction. Typically, HEK 293 cells stably expressing the wild-type hERG channel are used in whole-cell patch-clamp electrophysiology experiments. Cells are voltage-clamped, and the hERG current (IHERG) is elicited by a standard voltage protocol. Lidoflazine is applied at increasing concentrations, and the inhibition of the peak tail current is measured to construct a concentration-response curve. The IC50 for hERG blockade is then calculated, with Lidoflazine showing an IC50 of approximately 16 nM.
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| Cell Assay |
Cellular assays for Lidoflazine are performed in HEK 293 cells stably expressing the hERG potassium channel. Cells are cultured under standard conditions and plated in recording chambers for electrophysiological studies. Whole-cell patch-clamp recordings are conducted to measure the hERG current. Cells are exposed to varying concentrations of Lidoflazine, and the inhibition of the hERG current is quantified. These assays are critical for evaluating the proarrhythmic potential of the compound and are a standard part of cardiac safety pharmacology screening.
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| Animal Protocol |
In vivo animal models used to study Lidoflazine typically involve cardiovascular monitoring in rodents, dogs, or other mammalian species. The compound is administered via oral or intravenous routes, and its effects on electrocardiographic parameters, particularly the QT interval, are monitored. In conscious or anesthetized animals, the dose-dependent prolongation of the QT interval is measured to assess the compound's proarrhythmic risk. Additionally, coronary vasodilation and hemodynamic effects are evaluated to characterize its antianginal efficacy.
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| ADME/Pharmacokinetics |
Lidoflazine is soluble in DMSO at ≥10 mg/mL. It is stable as a powder when stored at 2-8°C. The compound is formulated for in vivo administration using vehicles such as DMSO, PEG300, Tween 80, and saline. However, detailed pharmacokinetic parameters such as half-life, bioavailability, volume of distribution, and clearance are not extensively reported in the available literature. As a lipophilic compound, it is expected to have good tissue penetration.
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| Toxicity/Toxicokinetics |
Lidoflazine carries a significant risk of QT interval prolongation and ventricular arrhythmias due to its high-affinity blockade of the hERG potassium channel. The IC50 for hERG blockade is <0.1 μM, approximately 16 nM. This potent hERG inhibition makes the compound a classic example of drug-induced cardiotoxicity. Comprehensive toxicology data, including acute and chronic toxicity studies, are not detailed in the available literature, but the cardiotoxic potential is well-recognized and has limited its clinical use.
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| References | |
| Additional Infomation |
2-[4-[4,4-bis(4-fluorophenyl)butyl]-1-piperazinyl]-N-(2,6-dimethylphenyl)acetamide is a diarylmethane compound. It has coronary artery vasodilatory effects and certain antiarrhythmic effects.
Lidoflazine is a research-grade compound not approved for clinical use in most countries due to its cardiotoxic profile. It is featured on the Calcium Channels page of the Handbook of Receptor Classification and Signal Transduction. The compound's primary application is as a pharmacological tool for studying calcium channel and hERG channel function. Its high-affinity hERG blockade makes it a valuable reference standard in cardiac safety pharmacology assays for evaluating the proarrhythmic potential of new chemical entities. |
| Molecular Formula |
C30H35F2N3O
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|---|---|
| Molecular Weight |
491.63
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| Exact Mass |
491.275
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| CAS # |
3416-26-0
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| PubChem CID |
3926
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| Appearance |
White to off-white solid powder
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| Density |
1.161g/cm3
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| Boiling Point |
632.6ºC at 760mmHg
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| Melting Point |
158-162ºC
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| Flash Point |
336.4ºC
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| Index of Refraction |
1.581
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| LogP |
5.698
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
623
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZBIAKUMOEKILTF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H35F2N3O/c1-22-5-3-6-23(2)30(22)33-29(36)21-35-19-17-34(18-20-35)16-4-7-28(24-8-12-26(31)13-9-24)25-10-14-27(32)15-11-25/h3,5-6,8-15,28H,4,7,16-21H2,1-2H3,(H,33,36)
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| Chemical Name |
2-[4-[4,4-Bis(4-fluorophenyl)butyl]piperazin-1-yl]-N-(2,6-dimethylphenyl)acetamide
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| Synonyms |
Lidoflazine KliniumOrdiflazine CorflazineClinium
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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 | 2.0340 mL | 10.1702 mL | 20.3405 mL | |
| 5 mM | 0.4068 mL | 2.0340 mL | 4.0681 mL | |
| 10 mM | 0.2034 mL | 1.0170 mL | 2.0340 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.
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