Tibenelast sodium

Modify Date: 2024-01-06 14:19:00

Tibenelast sodium Structure
Tibenelast sodium structure
Common Name Tibenelast sodium
CAS Number 105102-18-9 Molecular Weight 288.29500
Density N/A Boiling Point 440.8ºC at 760mmHg
Molecular Formula C13H13NaO4S Melting Point N/A
MSDS N/A Flash Point 220.4ºC

 Use of Tibenelast sodium


Tibenelast sodium is a phosphodiesterase inhibitor.

 Names

Name sodium,5,6-diethoxy-1-benzothiophene-2-carboxylate
Synonym More Synonyms

 Tibenelast sodium Biological Activity

Description Tibenelast sodium is a phosphodiesterase inhibitor.
Related Catalog
Target

phosphodiesterase[1]

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[1].
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[2].
References

[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.

 Chemical & Physical Properties

Boiling Point 440.8ºC at 760mmHg
Molecular Formula C13H13NaO4S
Molecular Weight 288.29500
Flash Point 220.4ºC
Exact Mass 288.04300
PSA 86.83000
LogP 2.06220
Vapour Pressure 1.52E-08mmHg at 25°C

 Synonyms

tibenelast sodium
unii-v58cn2sy21