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Epinastine/依匹斯汀 {[allProObj[0].p_purity_real_show]}

货号:A540909 同义名: WAL801

Epinastine is mast cell stabilizer and antihistamine that is used to treat allergic conjunctivitis.

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Epinastine/依匹斯汀 化学结构 CAS号:80012-43-7
Epinastine/依匹斯汀 化学结构
CAS号:80012-43-7
Epinastine/依匹斯汀 3D分子结构
CAS号:80012-43-7
Epinastine/依匹斯汀 化学结构 CAS号:80012-43-7
Epinastine/依匹斯汀 3D分子结构 CAS号:80012-43-7
规格 价格 会员价 库存 数量
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Epinastine/依匹斯汀 纯度/质量文件 产品仅供科研

货号:A540909 标准纯度: {[allProObj[0].p_purity_real_show]}
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Epinastine/依匹斯汀 生物活性

描述 Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine shows a high affinity to H1-receptors in receptor binding studies in the guinea pig ileum. Epinastine inhibits histamine-induced reactions in the skin or the lung of rats, dogs and guinea pigs[3]. Epinastine is able to displace specific [3H]NC-5Z binding at low concentrations in the locust nervous tissue. Epinastine binds to the honey bees neuronal octopamine receptor with Ki of 1.1 nM. Epinastine antagonises octopamine-induced cAMP formation in the insect brain. Epinastine could serve as a highly specific antagonist of octopamine receptors that enables physiological dissection of octopaminergic neurotransmission within the nervous system of insects[4]. Epinastine was similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. The drug was effective in inhibiting not only Ca2+ uptake into lung mast cells in actively sensitized guinea pigs but also Ca2+ release from the intracellular Ca store of rat peritoneal mast cells exposed to both compound 48/80 and substance P. No significant changes were observed in phosphodiesterase activity in rat peritoneal mast cells treated with epinastine, while adenylate cyclase activity was augmented by epinastine[5]. Epinastine shows a dose- and time-dependent suppressive effect on IL-8, one of the chemokines for eosinophils, released from eosinophils isolated from atopic diseases. Epinastine might prevent the autocrine cycle for recruitment of human eosinophils by inhibiting IL-8 release from these cells[6].

Epinastine/依匹斯汀 参考文献

[1]Fugner A, Bechtel WD, et al. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung. 1988 Oct;38(10):1446-53.

[2]Roeder T, Degen J, et al. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol. 1998 May 22;349(2-3):171-7.

[3]Fügner A, Bechtel WD, Kuhn FJ, Mierau J. In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung. 1988 Oct;38(10):1446-53

[4]Roeder T, Degen J, Gewecke M. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol. 1998 May 22;349(2-3):171-7

[5]Kamei C, Akagi M, Mio M, Kitazumi K, Izushi K, Masaki S, Tasaka K. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205

[6]Kohyama T, Takizawa H, Akiyama N, Sato M, Kawasaki S, Ito K. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun. 1997 Jan 3;230(1):125-8

Epinastine/依匹斯汀 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.06mL

4.01mL

2.01mL

40.11mL

8.02mL

4.01mL

Epinastine/依匹斯汀 技术信息

CAS号80012-43-7
分子式C16H15N3
分子量 249.31
SMILES Code NC1=NCC2N1C3=CC=CC=C3CC4=CC=CC=C24
MDL No. MFCD00865648
别名 WAL801
运输蓝冰
InChI Key WHWZLSFABNNENI-UHFFFAOYSA-N
Pubchem ID 3241
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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