Tibenelast sodium (Synonyms: LY 186655)
目录号: PL09654 纯度: ≥99%
Tibenelast sodium 是一种磷酸二酯酶 (phosphodiesterase) 抑制剂。
CAS No. :105102-18-9
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中文名称
Tibenelast sodium
中文别名
硫苯司特
英文名称
Tibenelast sodium
英文别名
Benzo[b]thiophene-2-carboxylicacid, 5,6-diethoxy-, sodium salt (1:1);sodium,5,6-diethoxy-1-benzothiophene-2-carboxylate;AC1Q1V6M;CHEMBL2107210;LY 186655;LY-186655;sodium 5,6-diethoxybenzo(b)thiophene-2-carboxylate;SureCN635432;TIBENELAST SODIUM;Tibenelast sodium (USAN);Tibenelast sodium [USAN];UNII-V58CN2SY21
Cas No.
105102-18-9
分子式
C13H13O4S-.Na+
分子量
288.29
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Tibenelast sodium 是一种磷酸二酯酶 (phosphodiesterase) 抑制剂。
生物活性
Tibenelast sodium is a phosphodiesterase inhibitor.
性状
Solid
IC50 & Target[1][2]
phosphodiesterase
体外研究(In Vitro)
The effect of the phosphodiesterase inhibitor Tibenelast, and placebo on isoproterenol-induced changes in heart rate, cAMP and norepinephrine levels in normal male volunteers is studied. Tibenelast increases the heart rate response to isoproterenol infusion, whereas norepinephrine and cAMP levels are not different in any treatment. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Tibenelast is a potent orally active compound against anaphylactic shock induced by high dose antigen aerosol. When a lower aerosol challenge (0.05 mg/mL) is employed, bronchoconstriction is observed with a concomitant increase in lung resistance (RL) and a fall in dynamic compliance (Cdyn). Tibenelast at 25 mg/kg p.o. prevents these changes. Tibenelast is 10 times more potent than Aminophylline by i.v. administration; normalization of pulmonary function is achieved at 1 mg/kg i.v. Tibenelast is synergistic with epinephrine. The oral dose response curve of Tibenelast is enhanced with the co-administration of epinephrine. Tibenelast may be of significant value in the treatment of asthma and other respiratory diseases. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Schwertschlag US, et al. Effect of tibenelast (a phosphodiesterase inhibitor) and theophylline on isoproterenol-stimulated heart rate, cyclic AMP and norepinephrine levels. Pharmacology. 1993;46(3):142-7.
[2]. Ho PP, et al. Tibenelast, 5,6-diethoxybenzo(B)thiophene-2-carboxylic acid, sodium salt (LY186655), is an orally active anti-asthma compound in the guinea pig. Life Sci. 1990;46(13):917-25.
溶解度数据
In Vitro: DMSO : 50 mg/mL (173.44 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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