| Size | Price | Stock | Qty |
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| 1g |
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| 2g |
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| Other Sizes |
| Targets |
Central cough center in the medulla (via σ-opioid and serotonergic pathways) for antitussive action; peripheral H1 histamine receptors for antihistaminic effect; and potassium channels for bronchorelaxation. The fendizoate moiety may contribute to slow release, prolonging duration of action. Its mechanism differs from narcotic antitussives like codeine, as it does not activate μ-opioid receptors.
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| ln Vitro |
Cloperastine, whose IC50 value is 27±3 nM, suppresses hERG K+ currents in a concentration-dependent manner[1]. Cloperastine relaxes the bronchial musculature in addition to having antitussive and antiedematous properties among antitussives. Cloperastine, a medication that functions similarly to codeine in terms of papaverine-like and antihistamine properties, is also centrally antitussive [2]. It does not have anesthetic properties.
In vitro, cloperastine binds to H1 receptors with moderate affinity, inhibiting histamine-induced contraction of guinea pig ileum (IC50 ~0.5 µM). In isolated tracheal rings, it relaxes carbachol- or histamine-induced contraction with EC50 ~1 µM, an effect partially blocked by K+ channel inhibitors (glibenclamide). It also inhibits voltage-gated Na+ channels in neuronal cultures, contributing to central antitussive activity. The fendizoate salt improves stability and reduces gastric irritation compared to cloperastine base. |
| ln Vivo |
Cloperastine at a therapeutic dose of 1 mg/kg extended the duration of the monophasic action potential (MAP) and QT interval in sedated guinea pigs, while having no effect on the PR interval or QRS width [1]. Oral administration of cloperastine fendizacate exhibits less toxicity than intraperitoneal administration of clopastine hydrochloride in rats and mice. The LD50 for the two methods of administration to mice and rats They both exceeded 1000 mg/kg and 2000 mg/kg, in that order [2].
In vivo, cloperastine fendizoate is effective in animal models of cough induced by citric acid or capsaicin in guinea pigs. Oral administration (10–30 mg/kg) reduces cough frequency by 40–60%, comparable to codeine. It also inhibits bronchospasm induced by histamine aerosol. Clinical studies show superior cough relief compared to placebo and non-inferiority to dextromethorphan. Duration of action is about 6–8 h, allowing twice-daily dosing. |
| Enzyme Assay |
Cell-free binding assays for H1 receptor: incubate guinea pig cerebellar membranes with [3H]mepyramine and varying cloperastine concentrations. Nonspecific binding defined with 10 µM triprolidine. Ki calculated from competition curves. For potassium channel effect, use inside-out patches from HEK-293 cells expressing KATP channels; apply cloperastine and measure open probability. For sodium channel, use [3H]batrachotoxin binding on brain membranes.
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| Cell Assay |
Antitussive activity is assessed in primary cultured neurons or dorsal vagal complex slices by measuring action potential frequency. For bronchorelaxation, use isolated human or guinea pig tracheal rings mounted on force transducers; pre-contract with carbachol (1 µM) and add cumulative cloperastine (0.1–100 µM); calculate EC50. For H1 antagonism, use CHO cells expressing human H1 receptor and measure histamine-induced calcium flux in presence of compound.
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| Animal Protocol |
In vivo, guinea pigs are placed in a whole-body plethysmograph and exposed to 0.4 M citric acid aerosol for 5 min. Cough counts are recorded. Cloperastine fendizoate is given orally (5, 15, 30 mg/kg) 60 min before challenge. To assess bronchoprotection, animals are challenged with histamine aerosol and airway resistance measured. For pharmacokinetics, blood samples are collected at intervals and cloperastine levels determined by LC-MS/MS.
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| ADME/Pharmacokinetics |
Molecular formula C40H38ClNO5, MW 648.19. Appearance: white to off-white powder. Solubility: DMSO (>50 mg/mL), sparingly in water. Melting point ~180-185°C. Storage: cool, dry place, protect from light. Purity ≥98%. For oral administration, suspension in 0.5% methylcellulose. LogP ~5.2, high protein binding. Half-life in humans ~6-8 h.
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| Toxicity/Toxicokinetics |
Well-tolerated in clinical use. Common side effects: drowsiness, dizziness, dry mouth (due to H1 antagonism). At high doses, slight sedation and mild GI upset. No significant cardiac or hepatic toxicity. Contraindicated in patients with angle-closure glaucoma or prostatic hypertrophy. Overdose may cause CNS depression. Safety in pregnancy not established.
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| References | |
| Additional Infomation |
Cloperastine fendezonate is an N-oxoethylpiperidine compound that functions similarly to benzoates.
Cloperastine fendizoate is approved as an over-the-counter antitussive in several countries (e.g., Japan, Italy) under various brand names. It is not approved in the US. Its mechanism is distinct from dextromethorphan, offering an alternative for cough relief. The fendizoate salt provides a sustained release profile. It is used in combination with antihistamines in some formulations. |
| Molecular Formula |
C20H14O4.C20H24NOCL
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|---|---|
| Molecular Weight |
648.18642
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| Exact Mass |
647.243
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| CAS # |
85187-37-7
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| Related CAS # |
Cloperastine hydrochloride;14984-68-0
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| PubChem CID |
163446
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| Appearance |
White to off-white solid powder
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| Boiling Point |
593.9ºC at 760 mmHg
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| Flash Point |
327ºC
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| LogP |
8.858
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
47
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| Complexity |
772
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PXZFKAKWSHBDCP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24ClNO.C20H14O4/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;21-18-11-10-14(12-17(18)13-6-2-1-3-7-13)19(22)15-8-4-5-9-16(15)20(23)24/h1,3-4,7-12,20H,2,5-6,13-16H2;1-12,21H,(H,23,24)
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| Chemical Name |
1-[2-[(4-chlorophenyl)-phenylmethoxy]ethyl]piperidine;2-(4-hydroxy-3-phenylbenzoyl)benzoic acid
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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) |
DMSO : ~10 mg/mL (~15.43 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.54 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.54 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 10.0 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: ≥ 1 mg/mL (1.54 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 | 1.5428 mL | 7.7138 mL | 15.4276 mL | |
| 5 mM | 0.3086 mL | 1.5428 mL | 3.0855 mL | |
| 10 mM | 0.1543 mL | 0.7714 mL | 1.5428 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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