[145739-56-6]    

MFCD00936868

Synonyms : 6-(2-(3,4-Diethoxyphenyl)thiazol-4-yl)picolinic acid; OPC6535

Applications : Tetomilast is a novel thiazole phosphodiesterase-4 (PDE-4) inhibitor, which may prove useful in both the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD). The pharmacological profile of Tetomilast revealed an IC50 value of 380 nM, which is weaker than those of Roflumilast and Cilomilast. Moreover, it has a long half-life (approximately 24h) and high bioavailability (nearly 100%), which are better than those of Roflumilast and Cilomilast. These data support Tetomilast as a suitable once-daily orally administered candidate.

References : Mulhall A. M. et al.: Expert Opin. Invest. Drugs 24, 1597-1611, 2015; Ti H. et al.: J. Med. Chem., 62(13), 5944-5978, 2019.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.