Ebastine (Synonyms:依巴斯汀; LAS-W 090; RP64305)
目录号 : KM14004 CAS No. : 90729-43-4 纯度 : 98%

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。

规格 价格 是否有货 数量
500mg
In-stock
1g
In-stock
5g
In-stock
10g 询价 In-stock
50g 询价 In-stock

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生物活性

Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.

体外研究

Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC.
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.

Cell Proliferation Assay

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

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.
体内研究

In rats, after intravenous administration of [C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t1/2 α) of 1.6 h and β-phase half-life (t1/2 β) of 3.1 h.
Following oral administration of [C]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 t1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with Cmax of 1110 ng eq./ml at 4 h and with t1/2 of 4.0 h.

分子式
C32H39NO2
分子量
469.66
CAS号
90729-43-4
中文名称
依巴斯汀;艾巴斯啶
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
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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