Mizolastine dihydrochloride
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial.
For research use only. We do not sell to patients.
- CAS No.: 1056596-82-7
- Formula: C24H27Cl2FN6O
- Molecular Weight:505.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Mizolastine dihydrochloride (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells[1].
Mizolastine dihydrochloride (0.1 µM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mast cells (from Kunming mice)
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Concentration:1-10000 nM
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Incubation Time:0.5-6 h
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Result:Markedly inhibited release of KC, VEGF and TNF-α in a time- and dose- dependent manner.
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Cell Line:Mast cells (from Kunming mice)
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Concentration:0.1 µM
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Incubation Time:4 h
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Result:Led to a significant reduction of induced VEGF165, VEGF120, TNF-α and KC mRNA synthesis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (specific-pathogen-free; 234-254 g; 7 to 8-week-old; rat paw edema model)[2].
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Dosage:0.3 mg/kg
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Administration:Oral gavage; single daily for 7 days.
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Result:Significantly reduced paw edema by 21% at 1 h, and by 14‑18% between 2 and 4 h.
Inhibited inflammatory cell infiltration and significantly reduced levels of LTB4.
Suppressed expression of 5‑LOX, cPLA2, FLAP and LTB4r mRNA.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1056596-82-7
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Molecular Weight 505.42
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Formula C24H27Cl2FN6O
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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 [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mizolastine dihydrochloride Related Classifications
HY-B0164A Related Classifications
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