DGAT1 Inhibitor

DGAT1-IN-4 is a potent, orally active, and selective DGAT1 inhibitor with an IC₅₀ of 17 nM. DGAT1-IN-4 exhibits >588-fold selectivity over DGAT2. DGAT1-IN-4 suppresses intracellular triglyceride synthesis in mouse myoblast cells. DGAT1-IN-4 suppresses body weight gain in diet-induced obese dogs. DGAT1-IN-4 can be used for the research of obesity.

Ent-Calquiquelignan E (Compound 8) is a flavonoid lignan compound. Ent-Calquiquelignan E can selectively inhibit diacylglycerol acyltransferase 1 (DGAT1) with an IC₅₀ of 71.5 μM. Ent-Calquiquelignan E can be used for the research of metabolic diseas.

Ldalaptican pegol (AON-D21; NOX-D21) is a PEGylated mixed RNA/DNA L-aptamer that specifically binds to complement C5a. Ldalaptican pegol binds to C5a and the C5a moiety on uncleaved C5, thereby blocking C5a signaling. This inhibition suppresses downstream inflammatory responses, immune cell infiltration and chemotaxis, the release of pro-fibrotic factors, and abnormalities in lipid metabolism signaling pathways. Ldalaptican pegol can also alleviate allograft rejection. Ldalaptican pegol can be used in research on inflammatory muscle diseases, Duchenne muscular dystrophy (DMD), diabetes, renal fibrosis, and allograft organ transplant rejection.