IC50: 72 nM (Rat D5D), 22 nM (Human D5D)

D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC ₅₀ s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity.

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