产品
编 号：F461971
分子式：C26H30ClFN2O2
分子量：456.98
分子式：C26H30ClFN2O2
分子量：456.98
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 79547-78-7
产品详情
生物活性：
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
体内研究：
Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) hydrochloride inhibits the virus-induced airway hyperresponsiveness.Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior.Levocabastine (500 μg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4.Animal Model:Guinea-pig with Parainfluenza-3 (PI-3) virus
Dosage:0.25 mg/kg
Administration:Intraperitoneal injection; twice a day for five days
Result:Suppressed the influx of broncho-alveolar cells and increased in albumin content.
Animal Model:Male C57BL/6J mice (8-9 weeks old)
Dosage:0.05 mg/kg; 30 mg/kg (β-LT)
Administration:Intraperitoneal injection; once
Result:Blocked the anxiolytic effect ofβ-LT and decreased the number of head-dips.
Animal Model:Ovalbumin-sensitized guinea pigs
Dosage:500 μg/eye
Administration:drops eye, once
Result:Produced a noteworthy protection from allergic conjunctivitis (AC) and prevented the conjuctival elevation of VLA-4 as well as conjunctival eosinophil infiltration.
体外研究：
Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of 125I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC50 of 406.2μm. Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) hydrochloride inhibits α4β1 integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits α4β1 integrindependent adhesion of Jurkat cells to VCAM-1 with an IC50 of 395.6 μM, and the adhesion of EoL-1 cells with an IC50 of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC50=443.7 μM).
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
体内研究：
Levocabastine (R 50547; 0.25 mg/kg; i.p.; twice a day for five days; guinea-pig with Parainfluenza-3 (PI-3) virus) hydrochloride inhibits the virus-induced airway hyperresponsiveness.Levocabastine (0.05 mg/kg; i.p.; once; male C57BL/6J mice) hydrochloride blocks anti-stress effect ofβ-LT on mouse behavior.Levocabastine (500 μg/eye; drops eye; once; ovalbumin-sensitized guinea pigs) hydrochloride induces allergic conjunctivitis (AC) and a significant increase of conjunctival VLA-4.Animal Model:Guinea-pig with Parainfluenza-3 (PI-3) virus
Dosage:0.25 mg/kg
Administration:Intraperitoneal injection; twice a day for five days
Result:Suppressed the influx of broncho-alveolar cells and increased in albumin content.
Animal Model:Male C57BL/6J mice (8-9 weeks old)
Dosage:0.05 mg/kg; 30 mg/kg (β-LT)
Administration:Intraperitoneal injection; once
Result:Blocked the anxiolytic effect ofβ-LT and decreased the number of head-dips.
Animal Model:Ovalbumin-sensitized guinea pigs
Dosage:500 μg/eye
Administration:drops eye, once
Result:Produced a noteworthy protection from allergic conjunctivitis (AC) and prevented the conjuctival elevation of VLA-4 as well as conjunctival eosinophil infiltration.
体外研究：
Levocabastine (0-1000 μM; HEK-293 cells) hydrochloride causes inhibition of 125I-FN binding to the SPA bead-associated α4β1 integrin in a concentration-dependent manner with an IC50 of 406.2μm. Levocabastine (0-1000 μM; 30 min; Jurkat cells and EoL-1 cells) hydrochloride inhibits α4β1 integrin/VCAM-1-mediated cell adhesion in vitro. Levocabastine inhibits α4β1 integrindependent adhesion of Jurkat cells to VCAM-1 with an IC50 of 395.6 μM, and the adhesion of EoL-1 cells with an IC50 of 403.6 μM. Moreover, Levocabastine inhibits adhesion of human eosinophils to VCAM-1-coated wells (IC50=443.7 μM).
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