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Prostaglandins have a short life in vivo because NAD+-dependent 15-hydroxy prostaglandin dehydrogenase (15-PGDH) catalyzes their oxidation to 15-keto metabolites with greatly reduced biological activity.1 Thiazolidinediones (TZDs) are a class of PPARγ agonists that have potent 15-PGDH inhibitory activity.2,3 CAY10638 is a TZD derivative that inhibits 15-PGDH activity with an IC50 value of 31 nM.3
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1. 15-
2. Thiazolidinediones. An pharmacological overview. Clin. Drug Investig. 22(8), 485-505 (2002).
3. Synthesis and SAR of thiazolidinedione derivatives as 15-