| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Verapamil EP Impurity C hydrochloride targets the same pathways as the parent compound verapamil, including calcium channels, P-glycoprotein (P-gp), and cytochrome P450 enzymes. Verapamil is a calcium channel blocker that inhibits L-type calcium channels in cardiac and vascular smooth muscle. It is also a potent first-generation P-glycoprotein (P-gp) inhibitor. As an impurity, this compound may exhibit similar but not identical biological activities to verapamil, though its specific receptor binding profile has not been extensively characterized.
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| ln Vitro |
In vitro studies of Verapamil EP Impurity C hydrochloride are limited, as the compound is primarily used as an analytical reference standard rather than a pharmacological tool. The impurity may retain some calcium channel blocking activity similar to verapamil, though with potentially different potency due to structural differences. Standard in vitro assays for calcium channel blockers include patch-clamp electrophysiology on cardiomyocytes or cell lines expressing L-type calcium channels, as well as functional assays measuring calcium influx using fluorescent indicators. The compound's activity against P-glycoprotein may also be assessed using efflux assays in cell lines overexpressing P-gp.
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| ln Vivo |
In vivo studies of Verapamil EP Impurity C hydrochloride are not typically conducted, as the compound is used as an impurity standard rather than a therapeutic agent. If studied, the compound would be expected to exhibit some degree of calcium channel blocking activity and P-gp inhibition similar to verapamil. Verapamil itself is well-characterized in vivo, showing antihypertensive, antianginal, and antiarrhythmic effects through L-type calcium channel blockade. Animal models used for verapamil include spontaneously hypertensive rats and various models of cardiac arrhythmia. The impurity would likely have reduced potency compared to the parent compound.
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| Enzyme Assay |
For non-cell-based receptor binding assays, Verapamil EP Impurity C hydrochloride can be evaluated using membrane preparations from tissues expressing L-type calcium channels. Radioligand binding displacement experiments are performed using a radiolabeled calcium channel ligand such as [3H]-verapamil or [3H]-nitrendipine. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 1-2 hours. Bound radioligand is separated from free by filtration through glass fiber filters. Nonspecific binding is determined in the presence of excess unlabeled verapamil. IC50 or Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing L-type calcium channels or P-glycoprotein are cultured in appropriate medium. For calcium channel activity, cells are loaded with calcium-sensitive fluorescent dyes such as Fluo-4 AM. After pre-incubation with various concentrations of the test compound, calcium influx is stimulated by depolarization with high potassium buffer. Fluorescence is measured using a plate reader. For P-gp activity, assays using calcein-AM accumulation in P-gp-expressing cell lines can be performed. Cells are incubated with the test compound and calcein-AM, and intracellular fluorescence is measured. Increased fluorescence indicates P-gp inhibition.
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| Animal Protocol |
In vivo animal studies for Verapamil EP Impurity C hydrochloride are not standard practice, as this compound is an impurity reference standard. If evaluated, the compound would likely be administered to rodents via oral gavage or intravenous injection, similar to verapamil. Cardiovascular parameters including blood pressure, heart rate, and ECG would be monitored. The compound's ability to inhibit calcium channels in vivo could be assessed in models of hypertension or cardiac arrhythmia. However, given that this is an impurity rather than a therapeutic agent, comprehensive in vivo characterization is rarely performed.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Verapamil EP Impurity C hydrochloride would be expected to resemble those of verapamil, though the specific profile has not been characterized. Verapamil has an oral bioavailability of approximately 20-35% due to extensive first-pass metabolism, a plasma protein binding of about 90%, and a half-life of 3-7 hours. It is metabolized primarily by CYP3A4 in the liver. The impurity is soluble in DMSO at 62.5 mg/mL and can be formulated for in vitro studies. For research use, the compound should be stored at 4°C in sealed containers away from moisture.
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| Toxicity/Toxicokinetics |
The toxicity profile of Verapamil EP Impurity C hydrochloride is not well-documented, as it is a reference standard and impurity rather than a therapeutic compound. As a verapamil-related impurity, it may share some of the pharmacological effects of verapamil, including potential cardiovascular effects such as hypotension, bradycardia, and atrioventricular block at high concentrations. The compound is intended for research use only and not for human consumption. Standard safety precautions should be observed when handling the compound, including appropriate personal protective equipment and proper ventilation.
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| References | |
| Additional Infomation |
Verapamil EP Impurity C hydrochloride (NSC-609249 hydrochloride) is a reference standard used in pharmaceutical quality control for the analysis of verapamil drug substance and finished products. Verapamil is a calcium channel blocker approved for the treatment of hypertension, angina pectoris, and cardiac arrhythmias. It is also a potent P-glycoprotein inhibitor. The EP Impurity C designation indicates that this compound is recognized as a specified impurity in the European Pharmacopoeia monograph for verapamil. The compound is used in HPLC and other analytical methods to ensure the purity and safety of verapamil pharmaceutical products.
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| Molecular Formula |
C12H20CLNO2
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|---|---|
| Molecular Weight |
245.75
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| Exact Mass |
245.118
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| CAS # |
51012-67-0
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| PubChem CID |
355505
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
16
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| Complexity |
173
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCC1=CC(=C(C=C1)OC)OC.Cl
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| InChi Key |
YKFNIODBMIRAKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H19NO2.ClH/c1-13(2)8-7-10-5-6-11(14-3)12(9-10)15-4;/h5-6,9H,7-8H2,1-4H3;1H
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| Chemical Name |
2-(3,4-dimethoxyphenyl)-N,N-dimethylethanamine;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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: 62.5 mg/mL (254.32 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0692 mL | 20.3459 mL | 40.6918 mL | |
| 5 mM | 0.8138 mL | 4.0692 mL | 8.1384 mL | |
| 10 mM | 0.4069 mL | 2.0346 mL | 4.0692 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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