D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice.

Δ5D:72 nM, Δ5D (human):22 nM

D5D-IN-326 (10 mg/kg, p.o. for 6 weeks) also obviously decreases gene expression levels of Ccl2, Cd68, Adgre1, and Il6, decreases epididymal Lep and Adipoq mRNAs which are significantly increased in HFD DIO mice. D5D-IN-326 (0.1, 1, and 10 mg/kg, p.o. for 6 weeks) gradually decreases body weight at 10 mg/kg. However, it lowers doses are not effective in DIO mice after treatment for 6 weeks.