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Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 g | $35 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $39 | In Stock | In Stock |
| Description | Cloperastine fendizoate (Hustazol) inhibits the hERG K+ currents in a concentration-dependent manner (IC50: 27 nM). |
| Targets&IC50 | K+ current:27 nM |
| In vitro | Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also relaxes the bronchial musculature. Cloperastine is also endowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects [2]. |
| In vivo | In anesthetized guinea pigs, a therapeutic dose (1 mg/kg) of Cloperastine extended the QT interval and monophasic action potential duration, without altering the PR interval or QRS width [1]. When administered intraperitoneally, Cloperastine hydrochloride exhibits relatively low acute toxicity in rats and mice. As Cloperastine fendizoate, its oral administration demonstrates minimal toxicity, with LD50 values exceeding 1000 and 2000 mg/kg in rats and mice, respectively [2]. |
| Synonyms | Hustazol |
| Molecular Weight | 648.19 |
| Formula | C40H38ClNO5 |
| Cas No. | 85187-37-7 |
| Smiles | Clc1ccc(cc1)C(OCCN1CCCCC1)c1ccccc1.OC(=O)c1ccccc1C(=O)c1ccc(O)c(c1)-c1ccccc1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 8 mg/mL (12.34 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.54 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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