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 die

Δ5D:72 nM, Δ5D (human):22 nM

D5D-IN-326 administered orally at a dose of 10 mg/kg for six weeks notably reduces the gene expression levels of Ccl2, Cd68, Adgre1, and Il6, as well as epididymal Lep and Adipoq mRNAs, which are significantly elevated in mice with diet-induced obesity (DIO) following a high-fat diet (HFD). Additionally, at a dosage of 10 mg/kg, D5D-IN-326 progressively decreases body weight over the same period. However, lower doses (0.1 and 1 mg/kg) prove ineffective in altering body weight or addressing DIO in mice after six weeks of treatment.