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Mizolastine 2HCl (SL-850324; Mizollen; SL 85.0324 dihydrochloride; Mistalin; SL 850324; Mistamine; Mizolastina) is a novel and potent histamine H1-receptor antagonist (IC50 = 47 nM) with the potential to be used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
ln Vitro |
Mast cells' production of VEGF, KC, and TNF-α is inhibited by mezolastine diHClide (1–10,000 nM; 0.5–6 h) [1]. In mast cells, mizolastine diHClide (0.1 µM; 4 h) dramatically lowers the expression of KC, TNF-α, VEGF165, and VEGF120 mRNA [1].
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ln Vivo |
In an AA-induced inflammation model, mizolastine diHClide (0.3 mg/kg; oral; once daily for 7 days) inhibits the 5 LOX AA (arachidonic acid) metabolite leukotriene B4 (LTB4) as well as 5-LOX, cytosolic PLA2 (cPLA2), 5-LOX expression of LOX activating protein, and LTB4 receptor mRNA [2].
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Cell Assay |
Cell viability assay [1]
Cell Types: Mast cells (from Kunming mice) Tested Concentrations: 1-10000 nM Incubation Duration: 0.5-6 h Experimental Results: The release of KC, VEGF and TNF-α was Dramatically time- and dose-dependent mode of inhibition. RT-PCR[1] Cell Types: Mast cells (from Kunming mice) Tested Concentrations: 0.1 µM Incubation Duration: 4 hrs (hours) Experimental Results: Caused significant reduction in induced VEGF165, VEGF120, TNF-α and KC mRNA synthesis. |
Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (specific pathogen-free; 234-254g; 7 to 8 weeks old; rat paw edema model) [2].
Doses: 0.3 mg/kg Route of Administration: po (oral gavage); single dose daily for 7 days. Experimental Results: Paw edema was Dramatically diminished by 21% within 1 hour and 14-18% within 2 to 4 hrs (hrs (hours)). Inhibits inflammatory cell infiltration and Dramatically reduces LTB4 levels. Inhibits the expression of 5-LOX, cPLA2, FLAP and LTB4r mRNA. |
References |
[1]. Xia Q, et al. The effect of mizolastine on expression of vascular endothelial cell growth factor, tumour necrosis factor-alpha and keratinocyte-derived chemokine in murine mast cells, compared with dexamethasone and loratadine. Clin Exp Dermatol. 2005 Mar
[2]. Ren X, et al. The anti-inflammatory effects of Yunnan Baiyao are involved in regulation of the phospholipase A2/arachidonic acid metabolites pathways in acute inflammation rat model. Mol Med Rep. 2017 Oct;16(4):4045-4053. [3]. Prakash A, et al. Mizolastine: a review of its use in allergic rhinitis and chronic idiopathic urticaria. BioDrugs. 1998 Jul;10(1):41-63. |
Molecular Formula |
C24H27CL2FN6O
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Molecular Weight |
505.415186166763
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CAS # |
1056596-82-7
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Related CAS # |
Mizolastine;108612-45-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1NC(N(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C)=NC=C1.Cl.Cl
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9786 mL | 9.8928 mL | 19.7855 mL | |
5 mM | 0.3957 mL | 1.9786 mL | 3.9571 mL | |
10 mM | 0.1979 mL | 0.9893 mL | 1.9786 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.