ACSL5-IN-1 (Compound A) is an ACSL5 inhibitor with body weight-reducing activity. ACSL5-IN-1 inhibits ACSL5, an enzyme linked to fatty acid metabolism. ACSL5-IN-1 reduces body weight in diet-induced obesity mice. ACSL5-IN-1 can be used for the research of obesity, metabolic dysfunction-associated steatohepatitis, metabolic syndrome, non-alcoholic fatty liver disease, type 2 diabetes, acute myeloid leukemia, colorectal cancer, and breast cancer [1].
In Vitro, Long-chain acyl-CoA synthetase family member 5 (ACSL5) is widely expressed in the liver, small intestine, adipose tissue, spleen, uterus, lung and skeletal muscle of mammals. ACSL5 catalyzes the conversion of long-chain fatty acids in the cytoplasm to acyl-CoA. These acyl-CoA molecules are subsequently used for the synthesis of complex lipids and other products in the endoplasmic reticulum, or enter mitochondria for γ-oxidation. Fatty acids catalyzed by ACSL5 include palmitic acid, palmitoleic acid, oleic acid and linoleic acid. Studies show that ACSL5 is involved in glucose and lipid metabolism, and may play an important role in metabolic disorders. For example, ACSL5-/- mice exhibit increased FGF21 levels in the liver and serum, reduced fat mass, improved insulin sensitivity, increased energy expenditure and delayed triglyceride absorption[1].
References:
[1]. Thomas Bernard LEVY, et al. Compounds and methods of their use. WO2025174957A1. 2025-02-13.
In Vitro, Long-chain acyl-CoA synthetase family member 5 (ACSL5) is widely expressed in the liver, small intestine, adipose tissue, spleen, uterus, lung and skeletal muscle of mammals. ACSL5 catalyzes the conversion of long-chain fatty acids in the cytoplasm to acyl-CoA. These acyl-CoA molecules are subsequently used for the synthesis of complex lipids and other products in the endoplasmic reticulum, or enter mitochondria for γ-oxidation. Fatty acids catalyzed by ACSL5 include palmitic acid, palmitoleic acid, oleic acid and linoleic acid. Studies show that ACSL5 is involved in glucose and lipid metabolism, and may play an important role in metabolic disorders. For example, ACSL5-/- mice exhibit increased FGF21 levels in the liver and serum, reduced fat mass, improved insulin sensitivity, increased energy expenditure and delayed triglyceride absorption[1].
References:
[1]. Thomas Bernard LEVY, et al. Compounds and methods of their use. WO2025174957A1. 2025-02-13.