9177. Tesaglitazar

Nomenclature

CAS number: 251565-85-2
(αS)-α-Ethoxy-4-[2-[4-[(methylsulfonyl)oxy]phenyl]ethoxy]benzenepropanoic acid; (S)-2-ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid; AZ-242; Galida (AstraZeneca).
C20H24O7S; mol wt 408.47.
C 58.81%, H 5.92%, O 27.42%, S 7.85%.

Description and references

Dual-acting peroxisome proliferator-activated receptor (PPAR) α and γ agonist. Prepn: K. Andersson, WO 9962872 (1999 to Astra); idem, US 6258850 (2001 to AstraZeneca). Crystal structure in complex with the PPARα and PPARγ ligand binding domains: P. Cronet et al., Structure 9, 699 (2001). Solid-phase extraction LC/MS/MS determn in plasma: H. Svennberg et al., J. Chromatogr. B 787, 231 (2003). Mechanism of action study: B. D. Hegarty et al., Endocrinology 145, 3158 (2004). Clinical pharmacokinetics: H. Ericsson et al., Drug Metab. Dispos. 32, 923 (2004). Clinical effects on lipid and glucose metabolism in hypertriglyceridaemia and abdominal obesity: B. Fagerberg et al., Diabetologia 48, 1716 (2005). Review of clinical development: N. Kamber, T. M. E. Davis, IDrugs 8, 927-935 (2005).

Chemical structure

Therapeutic Category

Antidiabetic.

Keywords

Antidiabetic