2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Acyltransferase
  5. DGAT1 Isoform

DGAT1

DGAT1

DGAT1 (diacylglycerol O-acyltransferase 1) catalyzes the terminal step of triacylglycerol (TAG) synthesis by esterifying diacylglycerol with fatty acyl-CoA at the endoplasmic reticulum, making it a central regulator of cellular lipid storage and lipid droplet formation[1]. Mechanistically, DGAT1 functions within the Kennedy pathway and contributes substantially to triglyceride turnover, fatty acid utilization, and metabolic homeostasis in multiple tissues, including intestine, adipose tissue, and heart[1][2]. In disease-related models, genetic or pharmacological modulation of DGAT activity alters triglyceride accumulation, fatty acid oxidation, endoplasmic reticulum stress responses, and susceptibility to diet-induced metabolic dysfunction, supporting its relevance to obesity, hepatic steatosis, and cardiometabolic disorders[2][3][4]. Compared with the closely related isoform DGAT2, DGAT1 and DGAT2 catalyze the same biochemical reaction but exhibit distinct physiological functions, tissue distributions, structural origins, and compensatory capacities despite jointly accounting for most mammalian TAG synthesis[2][5]. Experimental studies further demonstrate that DGAT1 uniquely contributes to protection against lipid-induced endoplasmic reticulum stress under high-fat dietary conditions, whereas DGAT2 is not essential for adipose triglyceride storage in several mouse models[3]. For research applications, selective DGAT inhibitors have been widely used to interrogate triglyceride synthesis pathways and evaluate therapeutic strategies targeting metabolic disease, although gastrointestinal tolerability has limited clinical development of several DGAT1-directed compounds[4].

DGAT1 Related Products (2):

Cat. No. Product Name Effect Purity
  • HY-153507
    DGAT1-IN-4
    		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.
  • HY-N16614
    Ent-Calquiquelignan E
    		Inhibitor
    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.