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Purity: ≥98%
Mizolastine (Mizollen; SL 85.0324; Mistalin; SL-850324; SL 850324; Mistamine; Mizolastina) is a histamine H1-receptor antagonist with anti-allergic effects. It has been used to treat hay fever (seasonal allergic rhinitis), hives, and other allergic reactions. It inhibits the histamine H1-receptor with an IC50 of 47 nM. A single daily dose of non-sedating antihistamine is mizolastine. It usually acts quickly and blocks H1 receptors. Just the binding of histamine to receptors is inhibited; mast cell release of histamine is not stopped. Tight lips and throat are possible side effects.
| Targets |
Histamine H1 receptor ( IC50 = 47 nM )
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| ln Vitro |
Mizolastine (1–10,000 nM; 0.5–6 h) inhibits the release of VEGF, KC, and TNF-α in mast cells[1].
Mizolastine (0.1 µM; 4 h) dramatically lowers the expression of KC, TNF-α, VEGF165, and VEGF120 mRNA in mast cells[1]. |
| ln Vivo |
Mizolastine (0.3 mg/kg; p.o.; once daily for 7 days) suppresses expression of 5-LOX, cytosolic PLA2 (cPLA2), 5-LOX-activating protein, and LTB4 receptor mRNA. It also inhibits production of the 5-LOX AA (arachidonic acid) metabolite leukotriene B4 (LTB4) in the AA-induced inflammation model[2].
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| Cell Assay |
Cell Line: Mast cells (from Kunming mice)
Concentration: 1-10000 nM Incubation Time: 0.5-6 h Result: Markedly inhibited release of KC, VEGF and TNF-α in a time- and dose- dependent manner. |
| Animal Protocol |
Male Sprague-Dawley rats (specific-pathogen-free; 234-254 g; 7 to 8-week-old; rat paw edema model)
0.3 mg/kg Oral gavage; single daily for 7 days. |
| References |
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| Molecular Formula |
C24H25FN6O
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|---|---|---|
| Molecular Weight |
432.49
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| Exact Mass |
432.21
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| Elemental Analysis |
C, 66.65; H, 5.83; F, 4.39; N, 19.43; O, 3.70
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| CAS # |
108612-45-9
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| Related CAS # |
Mizolastine dihydrochloride;1056596-82-7;Mizolastine-13C,d3
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| Appearance |
Solid powder
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| SMILES |
CN(C1CCN(CC1)C2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)F)C5=NC=CC(=O)N5
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| InChi Key |
PVLJETXTTWAYEW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H25FN6O/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)
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| Chemical Name |
2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methylamino]-1H-pyrimidin-6-one
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.78 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (5.78 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 25.0 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: ≥ 2.5 mg/mL (5.78 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 | 2.3122 mL | 11.5610 mL | 23.1219 mL | |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6244 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01928316 | Completed | Drug: Mizolastine (imported) Drug: Mizolastine domestic (made in China) |
Healthy | Xian-Janssen Pharmaceutical Ltd. | June 2009 | Phase 1 |
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