(±)-Tazifylline
(Synonyms: (±)-他齐茶碱) 目录号 : GC31026(±)-Tazifylline是一种有效的,选择性的长效组胺H1受体拮抗剂。
Cas No.:79712-55-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.
Tazifylline potently inhibits contractions evoked by stimulation of histamine H1-receptors in isolated guinea pig ilea and exhibits high affinity for these receptors in radioligand binding studies in vitro Tazifylline has much lower affinity for histamine H2-receptors, alpha- and beta-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. Tazifylline poorly inhibits the release of histamine from rat peritoneal mast cells[1].
In rats, guinea pigs and dogs the antihistaminic effect of Tazifylline is rapid in onset and long-lived. In anesthetized guinea pigs, Tazifylline markedly inhibits histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline is more potent in reducing the inflammatory effects of intradermal histamine than that evoked by anaphylactic reaction. In conscious dogs, orally administered Tazifylline inhibits histamine-induced skin inflammation for long periods of time and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1-receptors. Large oral doses of Tazifylline does not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats[1].
[1]. Poizot A, et al. Animal pharmacology of the selective histamine H1-receptor antagonist tazifylline. Arzneimittelforschung. 1986 Apr;36(4):695-702.
Cas No. | 79712-55-3 | SDF | |
别名 | (±)-他齐茶碱 | ||
Canonical SMILES | O=C(N1C)N(C)C2=C(N(CC(O)CN3CCN(CCCSC4=CC=CC=C4)CC3)C=N2)C1=O | ||
分子式 | C23H32N6O3S | 分子量 | 472.6 |
溶解度 | Soluble in DMSO | 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 | 2.116 mL | 10.5798 mL | 21.1595 mL |
5 mM | 0.4232 mL | 2.116 mL | 4.2319 mL |
10 mM | 0.2116 mL | 1.058 mL | 2.116 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。