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Tazanolast (TO 188) Sale

(Synonyms: 他扎司特; TO 188; Tazalest; Tazanol) 目录号 : GC31796

Tazanolast (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。

Tazanolast (TO 188) Chemical Structure

Cas No.:82989-25-1

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1mg
¥3,570.00
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5mg
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10mg
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20mg
¥21,420.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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.

产品描述

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.

Chemical Properties

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 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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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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