Ebastine (LAS-W 090) 是一种具有口服活性的第二代组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Ebastine 可用于过敏性鼻炎的症状和慢性特发性荨麻疹的研究。
| 生物活性 | Ebastine (LAS-W 090) is an orally active, second-generationhistamine H1 receptorantagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1]. |
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体外研究
(In Vitro) | Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC[2].
Ebastine (10-500 ng/mL; 24-48 hours) treatment shows dose-dependent increases in Cyclin D1, Cyclin E1, and Cyclin A expression levels. And the expression levels of Cdk4, Cdk2, and Cdc2 are alos increased. Ebastine treatment elevates expression levels of phospho-AKT and phospho-p44/42 extracellular signal-regulated kinase[2].
Cell Proliferation Assay[2] | Cell Line: | Human follicle dermal papilla cells (HFDPC) | | Concentration: | 10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL | | Incubation Time: | 24 hours, 48 hours | | Result: | The proliferative activity in cells was significantly enhanced. |
Western Blot Analysis[2] | Cell Line: | Human follicle dermal papilla cells (HFDPC) | | Concentration: | 10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL | | Incubation Time: | 24 hours | | Result: | The expression levels of cell-cycle regulatory proteins and an antiapoptotic protein were increased in HFDPC. |
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体内研究
(In Vivo) | In rats, after intravenous administration of [14C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t1/2α) of 1.6 h and β-phase half-life (t1/2β) of 3.1 h[3].
Following oral administration of [14C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (Cmax) of 102 ng eq./ml at 2 h and decreased monophasically with t1/2of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with Cmaxof 1110 ng eq./ml at 4 h and with t1/2of 4.0 h[3].
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: Ethanol : 58.75 mg/mL(125.09 mM;Need ultrasonic) DMSO : 8.33 mg/mL(17.74 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1292 mL | 10.6460 mL | 21.2920 mL | | 5 mM | 0.4258 mL | 2.1292 mL | 4.2584 mL | | 10 mM | 0.2129 mL | 1.0646 mL | 2.1292 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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