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| Other Sizes |
| Targets |
Cloperastine hydrochloride targets the hERG (human Ether-à-go-go-Related Gene) potassium channel, with an IC50 of 27 nM for inhibiting hERG K+ current in a concentration-dependent manner. As an anti-tussive agent, its primary mechanism of action involves central antitussive effects, likely through modulation of cough reflex pathways. The compound is a type of flavonoid.
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| ln Vitro |
Cloperastine, whose IC50 value is 27 nM, inhibits hERG K+ current in a concentration-inhibitory manner[1]. The antitussive drug cloperastine hydrochloride shortens ischemic tissue in addition to its antitussive and antiedematous properties. The medication cleopatrastine hydrochloride has antitussive central effects as well as antihistamine and papaverine-like activity that can provide comparable but non-narcotic effects [2].
In vitro, Cloperastine hydrochloride inhibits hERG K+ current with an IC50 of 27 nM in a concentration-dependent manner. This property is relevant for its cardiac safety profile, as hERG inhibition is associated with QT prolongation risk. The compound's anti-tussive activity has been demonstrated in preclinical models. |
| ln Vivo |
In anesthetized guinea pigs, cloperastine hydrochloride at a dose of 1 mg/kg prolongs the QT interval and monophasic action potential (MAP) duration without changing the PR interval or QRS width [1]. The intraperitoneal toxicity of cloperastine hydrochloride to mice and mice is relatively low, while the oral toxicity of cloperastine hydrochloride and findizole preparations is relatively low. Under the two routes, the LD50 of cloperastine hydrochloride in mice surpasses 1000 and 2000 mg/ kg[2].
In vivo, Cloperastine hydrochloride is used as an anti-tussive drug as an over-the-counter cold medicine. It is effective in suppressing cough in patients with respiratory conditions. The compound is available in oral formulations for symptomatic relief of cough. |
| Enzyme Assay |
The in vitro assay for Cloperastine hydrochloride involves measuring its inhibition of hERG potassium channel currents. Patch-clamp electrophysiology is performed on cells expressing the hERG channel. The compound is applied at varying concentrations, and the inhibition of hERG current is measured. The IC50 of 27 nM is determined from dose-response curves.
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| Cell Assay |
Cellular assays for Cloperastine hydrochloride are not typically performed for its anti-tussive activity, as it acts centrally. hERG inhibition assays are conducted using heterologous expression systems to assess cardiac safety.
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| Animal Protocol |
In vivo animal studies for Cloperastine hydrochloride are not detailed in the available sources. The compound is an approved anti-tussive drug. Preclinical studies would have been conducted in animal models of cough to assess efficacy and safety.
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| ADME/Pharmacokinetics |
Cloperastine hydrochloride is administered orally. It has a molecular weight of 366.33 g/mol. The compound is soluble in DMSO. It should be stored at room temperature in a cool, dry place. Specific PK parameters such as half-life, bioavailability, and clearance are not detailed in the available sources.
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| Toxicity/Toxicokinetics |
Cloperastine hydrochloride is generally well-tolerated. As an anti-tussive agent, common side effects may include drowsiness, dizziness, and gastrointestinal disturbances. The compound inhibits hERG K+ current with an IC50 of 27 nM, which may be associated with QT prolongation risk.
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| References | |
| Additional Infomation |
Cloperastine hydrochloride is a diarylmethane.
See also: Cloperastine (note moved to); Cloperastine fendizole (note moved to). Cloperastine hydrochloride is an over-the-counter anti-tussive drug used for the symptomatic relief of cough. It is available as a pharmaceutical product in various formulations. The compound is also available from chemical suppliers for research purposes. |
| Molecular Formula |
C20H25CL2NO
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|---|---|
| Molecular Weight |
366.3246
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| Exact Mass |
365.131
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| CAS # |
14984-68-0
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| Related CAS # |
Cloperastine fendizoate;85187-37-7
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| PubChem CID |
161104
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| Appearance |
White to off-white solid powder
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| Boiling Point |
84°C 35mm
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| Flash Point |
210.2ºC
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| Vapour Pressure |
2.15E-07mmHg at 25°C
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| Index of Refraction |
1.414
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| LogP |
5.671
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
318
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UNPLRYRWJLTVAE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24ClNO.ClH/c21-19-11-9-18(10-12-19)20(17-7-3-1-4-8-17)23-16-15-22-13-5-2-6-14-22;/h1,3-4,7-12,20H,2,5-6,13-16H2;1H
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| Chemical Name |
1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine;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 (e.g. under nitrogen), 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 : ~250 mg/mL (~682.46 mM)
H2O : ~100 mg/mL (~272.99 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.68 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 (5.68 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 (5.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (272.99 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7299 mL | 13.6493 mL | 27.2985 mL | |
| 5 mM | 0.5460 mL | 2.7299 mL | 5.4597 mL | |
| 10 mM | 0.2730 mL | 1.3649 mL | 2.7299 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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