Mizolastine dihydrochlorideHistamine H1-receptor antagonist CAS# 1056596-82-7 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1056596-82-7 | SDF | Download SDF |
| PubChem ID | 78358332 | Appearance | Powder |
| Formula | C24H27Cl2FN6O | M.Wt | 505.42 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | 2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methylamino]-1H-pyrimidin-6-one;dihydrochloride | ||
| SMILES | CN(C1CCN(CC1)C2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)F)C5=NC=CC(=O)N5.Cl.Cl | ||
| Standard InChIKey | VSBSKWNPRUHSSV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C24H25FN6O.2ClH/c1-29(23-26-13-10-22(32)28-23)19-11-14-30(15-12-19)24-27-20-4-2-3-5-21(20)31(24)16-17-6-8-18(25)9-7-17;;/h2-10,13,19H,11-12,14-16H2,1H3,(H,26,28,32);2*1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Mizolastine dihydrochloride Dilution Calculator
Mizolastine dihydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9786 mL | 9.8928 mL | 19.7855 mL | 39.571 mL | 49.4638 mL |
| 5 mM | 0.3957 mL | 1.9786 mL | 3.9571 mL | 7.9142 mL | 9.8928 mL |
| 10 mM | 0.1979 mL | 0.9893 mL | 1.9786 mL | 3.9571 mL | 4.9464 mL |
| 50 mM | 0.0396 mL | 0.1979 mL | 0.3957 mL | 0.7914 mL | 0.9893 mL |
| 100 mM | 0.0198 mL | 0.0989 mL | 0.1979 mL | 0.3957 mL | 0.4946 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Mizolastine dihydrochloride is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
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A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects.[Pubmed:11868924]
Ann Allergy Asthma Immunol. 2002 Feb;88(2):190-7.
BACKGROUND: Levocetirizine is the active enantiomer of cetirizine, a potent drug with little metabolism widely used for allergic rhinitis and urticaria. OBJECTIVE: This study compares the potency, consistency, onset, and duration of action of levocetirizine with other popular antihistamines. METHODS: Levocetirizine 5 mg, ebastine 10 mg, fexofenadine 180 mg, loratadine 10 mg, mizolastine 10 mg, or placebo in single doses were given to 18 healthy male volunteers in a double-blind, crossover, randomized fashion. Wheal-and-flare responses to epicutaneous histamine dihydrochloride (100 mg/mL) challenge were measured at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours after each dose. RESULTS: The overall effect of each drug was evaluated by the area under the curve (0 to 24 hours). Levocetirizine was the most potent and consistently effective drug for inhibiting the histamine-induced wheal-and-flare surface areas. Ebastine, fexofenadine, and mizolastine ranked next and had almost identical effects for inhibiting the wheal. Loratadine was the least potent drug. Levocetirizine, fexofenadine, and mizolastine inhibited the wheal-and-flare response after 1 hour and reached their peak for inhibition after 4 hours. Ebastine and loratadine could be distinguished from placebo only after 4 hours. After treatment with levocetirizine, all 18 subjects had >95% inhibition of the wheal response at one timepoint. Fexofenadine, mizolastine, and ebastine were inhibitory in declining order. All treatments were considered safe and well tolerated. CONCLUSIONS: Levocetirizine, the active enantiomer of cetirizine, is more potent and consistent than other popular H1 antihistamines for blocking the cutaneous response to histamine. These findings may predict the efficacy of this drug in treating allergic disorders.
