Mizolastine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mizolastine 是一种组胺 H1 受体拮抗剂，IC50 为 47 nM，用于治疗花粉热（季节性过敏性鼻炎）、荨麻疹和其他过敏反应。

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.

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 hResult: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.

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.

SL 85.0324 | Mistalin | Mistamine | Mizolastina

GPCR/G Protein

Histamine Receptor

H1 receptor

Inflammation/Immunology

——

108612-45-9

432.49

C24H25FN6O

>98% (HPLC)

Ethanol: <1 mg/mL warmed (<1 mM); Water: <1 mg/mL (<1 mM); DMSO: <1 mg/mL (<1 mM)

O=C1NC(N(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C)=NC=C1

2-((1-(1-(p-Fluorobenzyl)-2-benzimidazolyl)-4-piperidyl)methylamino)-4(3H)-pyrimidinone

(-20℃)

With Ice Pack

≥ 2 years