Tazanolast (TO 188)
(Synonyms: 他扎司特; TO 188; Tazalest; Tazanol) 目录号 : GC31796Tazanolast (TO 188) 是一种选择性肥大细胞稳定药物,对臭氧诱导的豚鼠气道高反应性有作用。
Cas No.:82989-25-1
Sample solution is provided at 25 µL, 10mM.
Tazanolast is a selective mast-cell-stabilizing drug, on ozone-induced airway hyperresponsiveness in guinea pigs.
Tazanolast, an orally active mast-cell-stabilizing drug, which has been shown to suppress passive cutaneous anaphylaxis, Schultz-Dale reaction in isolated tracheal muscle, and experimental asthma without antagonistic actions upon histamine- and leukotriene-D4-induced contraction, IgE-mediated or compound 48/80-induced histamine release from mast cells and lung fragments, compound 48/80-induced Ca2+ uptake into mast cells from extracellular medium, compound 48/80-induced translocation of protein kinase C from the cytosol to the membrane fraction of mast cells, and inositol trisphosphate production without directly inhibiting phospholipase C in mast cells[1].
Tazanolast administered before ozone exposure at doses of 30, 100, or 300 mg/kg inhibits ozone-induced airway hyperresponsiveness in a dose-dependent manner. Tazanolast administered after ozone exposure does not inhibit the airway hyperresponsiveness. Tazanolast does not significantly change the cell distribution of bronchoalveolar lavage (BAL) cells at 2 h after the exposure. Tazanolast significantly inhibits ozone-induced airway hyperresponsiveness in guinea pigs[1].
[1]. Igarashi A, et al. Tazanolast inhibits ozone-induced airway hyperresponsiveness in guinea pigs. Am J Respir Crit Care Med. 1998 May;157(5 Pt 1):1531-5.
Animal experiment: | Pigs[1] The 10 guinea pigs are also exposed to 2 ppm ozone for 2 h and then are orally administered 300 mg/kg of Tazanolast (T-300 post group). At 2 h after exposure PC200-MCh of each animal is determined. Thereafter, BAL is performed for each animal. On Day 1, preexposure PC200-MCh is determined for 50 guinea pigs. On Day 2, guinea pigs in groups of 10 are orally administered Tazanolast at a dose of 30 mg/kg (T-30 group), 100 mg/kg (T-100 group), or 300 mg/kg (T-300 group), or vehicle alone (vehicle group). After 30 min, the animals are exposed to 2 ppm ozone for 2 h. In addition, the other 10 guinea pigs are also exposed to 2 ppm ozone for 2 h and then are orally administered 300 mg/kg of Tazanolast (T-300 post group). At 2 h after exposure PC200-MCh of each animal is determined. Thereafter, BAL is performed for each animal. |
References: [1]. Igarashi A, et al. Tazanolast inhibits ozone-induced airway hyperresponsiveness in guinea pigs. Am J Respir Crit Care Med. 1998 May;157(5 Pt 1):1531-5. |
Cas No. | 82989-25-1 | SDF | |
别名 | 他扎司特; TO 188; Tazalest; Tazanol | ||
Canonical SMILES | O=C(OCCCC)C(NC1=CC=CC(C2=NN=NN2)=C1)=O | ||
分子式 | C13H15N5O3 | 分子量 | 289.29 |
溶解度 | DMSO : 66.67 mg/mL (230.46 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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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 | 3.4567 mL | 17.2837 mL | 34.5674 mL |
5 mM | 0.6913 mL | 3.4567 mL | 6.9135 mL |
10 mM | 0.3457 mL | 1.7284 mL | 3.4567 mL |
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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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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。
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