D5D-IN-326

D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC₅₀s 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 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice^[1]. IC50 & Target: IC50: 72 nM (Rat D5D), 22 nM (Human D5D)^[1] In Vitro: D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC₅₀s 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^[1]. In Vivo: 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^[1].
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^[1].