Epinastine (WAL801)
(Synonyms: 依匹斯汀; WAL801) 目录号 : GC31708
Epinastine (WAL801) (WAL801) 是一种抗组胺药和肥大细胞稳定剂。
Cas No.:80012-43-7
Sample solution is provided at 25 µL, 10mM.
Epinastine(WAL801) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.Target: Histamine ReceptorEpinastine 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 [1]. 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 [2]. Epinastine causes an inhibition of histamine release from rat peritoneal mast cells induced by both antigen-antibody reaction and compound 48/80. Epinastine is similarly effective in inhibiting compound 48/80-induced histamine release not only from isolated rat peritoneal mast cells but also from rat mesenterial pieces. Epinastine is 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 [3]. 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 [4].
[1]. Fugner, A., et al., In vitro and in vivo studies of the non-sedating antihistamine epinastine. Arzneimittelforschung, 1988. 38(10): p. 1446-53. [2]. Roeder, T., J. Degen, and M. Gewecke, Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. Eur J Pharmacol, 1998. 349(2-3): p. 171-7. [3]. Kamei, C., et al., 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): p. 191-205. [4]. Kohyama, T., et al., A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun, 1997. 230(1): p. 125-8.
Cas No. | 80012-43-7 | SDF | |
别名 | 依匹斯汀; WAL801 | ||
Canonical SMILES | NC1=NCC2N1C3=CC=CC=C3CC4=CC=CC=C24 | ||
分子式 | C16H15N3 | 分子量 | 249.31 |
溶解度 | DMSO : ≥ 50 mg/mL (200.55 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | 4°C, protect from light, stored under nitrogen |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 4.0111 mL | 20.0554 mL | 40.1107 mL |
5 mM | 0.8022 mL | 4.0111 mL | 8.0221 mL |
10 mM | 0.4011 mL | 2.0055 mL | 4.0111 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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