| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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Cloperastine fendizoate (Nitossil; Hustazol; Seki) is an antitussive, cough suppressant, and antihistamine agent acting as a σ1 receptor agonist, a GIRK channel blocker, a H1 receptor antagonist. It is approved and marketed as a cough suppressant in Japan, Hong Kong, and in some European countries.
| 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.
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|---|---|
| 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].
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| References | |
| Additional Infomation |
Cloperastine fendizoate is a N-oxyethylpiperidine. It is functionally related to a benzoate.
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| 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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