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Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 200 mg | $29 | In Stock | In Stock | |
| 500 mg | $35 | In Stock | In Stock | |
| 1 g | $48 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $39 | In Stock | In Stock |
| Description | Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative. |
| Targets&IC50 | H1 receptor:10 nM-19 nM |
| In vitro | In a tail-flick test, intraperitoneal injection of 12.5 mg/kg Hydroxyzine reduced the analgesic effect of morphine in rats; however, an injection of 50 mg/kg Hydroxyzine enhanced the effect of morphine. Furthermore, 500 μM Hydroxyzine significantly decreased the steady-state concentration of etoposide by half, achieving a concentration of 0.055 μM/mL in Sprague-Dawley rats. |
| In vivo | At a concentration of 0.1 mM, Hydroxyzine inhibits 50% of Experimental Autoimmune Encephalomyelitis (EAE) exacerbation in Lewis rats and suppresses 70% of mast cell degranulation. In bladder slices pre-treated with Hydroxyzine, a 60-minute incubation results in a 34% inhibition of 5-hydroxytryptamine release induced by 10 μM carbachol, with 1 μM Hydroxyzine causing a 25% inhibition and 0.1 μM suppressing it by 17%. Additionally, 500 μM Hydroxyzine significantly enhances the transport of digoxin to the serosal side in isolated everted jejunum sacs and notably reduces the efflux of approximately 2.4 μg/mL digoxin in the jejunum and ileum. |
| Synonyms | Hydroxyzine 2HCl |
| Molecular Weight | 447.83 |
| Formula | C21H27ClN2O2·2HCl |
| Cas No. | 2192-20-3 |
| Smiles | C1CN(CCN1CCOCCO)C(c1ccccc1)c1ccc(cc1)Cl.Cl.Cl |
| Relative Density. | 1.182 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 201 mM, Sonication is recommended. DMSO: 55 mg/mL (122.81 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO/H2O
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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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