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Mizolastine

SKU: orb1227011

Description

Mizolastine 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.(In Vitro):Mizolastine (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells.Mizolastine (0.1 μM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells.(In Vivo):Mizolastine (0.3 mg/kg; p.o.; single daily for 7 days) inhibits production of 5-LOX AA (arachidonic acid) metabolite leukotriene B4 (LTB4), and suppresses expression of 5-LOX, cytosolic PLA2 (cPLA2), 5-LOX-activating protein, and LTB4 receptor mRNA in the AA-induced inflammation model.

Images & Validation

Key Properties

CAS Number108612-45-9
MW432.49
Purity>98% (HPLC)
FormulaC24H25FN6O
SMILESO=C1NC(N(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C)=NC=C1
TargetHistamine Receptor
SolubilityEthanol: <1 mg/mL warmed (<1 mM); Water: <1 mg/mL (<1 mM); DMSO: <1 mg/mL (<1 mM)

Bioactivity

In Vivo
Mizolastine (0.3 mg/kg; p.o. ; single daily for 7 days) inhibits production of 5-LOX AA (arachidonic acid) metabolite leukotriene B4 (LTB4), and suppresses expression of 5-LOX, cytosolic PLA2 (cPLA2), 5-LOX-activating protein, and LTB4 receptor mRNA in the AA-induced inflammation model. Animal model: Male Sprague-Dawley rats (specific-pathogen-free; 234-254 g; 7 to 8-week-old; rat paw edema model). Dosage: 0.3 mg/kg. Administration: Oral gavage; single daily for 7 days. 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.
In Vitro
Mizolastine (1-10000 nM; 0.5-6 h) shows inhibitory effects on VEGF, KC and TNF-α release in mast cells. Mizolastine (0.1 μM; 4 h) significantly reduces VEGF165, VEGF120, TNF-α and KC mRNA expression in mast cells. Cell Viability 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. RT-PCR Cell line: Mast cells (from Kunming mice). Concentration: 0.1 μM Incubation time: 4 h. Result: Led to a significant reduction of induced VEGF165, VEGF120, TNF-α and KC mRNA synthesis.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SL 85.0324 | Mistalin | Mistamine | Mizolastina

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Mizolastine (orb1227011)

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