Bepotastine
(Synonyms: 贝他斯汀) 目录号 : GC39479A histamine H1 receptor antagonist
Cas No.:125602-71-3
Sample solution is provided at 25 µL, 10mM.
Bepotastine is an antagonist of the histamine H1 receptor that is selective over H3, α1-, α2-, and β-adrenergic, dopamine D2long, serotonin 5-HT2, muscarinic acetylcholine, and benzodiazepine receptors.1 It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED50 = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED50 = 3.2 ?g/kg).2,3 Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner.4 Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.
1.Kato, M., Nishida, A., Aga, Y., et al.Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate.Arzneimittelforschung.47(10)1116-1124(1997) 2.Murata, T., Matsumoto, Y., Suzuki, T., et al.Effect of betotastine besilate (TAU-284), a novel anti-allergic agent, on experimental allergic rhinitisArerugi46(7)576-584(1997) 3.Matsubara, S., Ono, C., Yamazaki, N., et al.Inhibitory effects of bepotastine, a novel anti-allergic drug on histamine-induced bronchoconstriction in anesthetized dogsYakuri to Chiryo25(4)895-900(1997) 4.Kida, T., Fuji, A., Sakai, O., et al.Bepotastine besilate, a highly selective histamine H1 receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis modelsExp. Eye Res.91(1)85-91(2010)
Cas No. | 125602-71-3 | SDF | |
别名 | 贝他斯汀 | ||
Canonical SMILES | O=C(O)CCCN1CCC(O[C@@H](C2=CC=C(Cl)C=C2)C3=CC=CC=N3)CC1 | ||
分子式 | C21H25ClN2O3 | 分子量 | 388.89 |
溶解度 | DMSO : 78mg/mL; Water : 30mg/mL (Need ultrasonic) | 储存条件 | Store at -20°C |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL |
5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL |
10 mM | 0.2571 mL | 1.2857 mL | 2.5714 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet