Niravoline (RU51599) is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. Niravoline has a pure water diuresis effect without associated electrolyte excretion. Niravoline can reduce brain oedema following transient forebrain ischaemia in rats.

MG16 is a prodrug of 10-Methoxycamptothecin. MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer.

Candicidin (≥50%) (Levorin (≥50%)) is an antifungal antibiotic. Candicidin (≥50%) exhibits potent antifungal activity against yeasts and yeast-like fungi, such as Candida albicans and Saccharomyces cerevisiae. Low concentrations of Candicidin (≥50%) do not adversely affect pea seed germination.

4-PSQ is an orally active neuroprotective agent. 4-PSQ possesses both antioxidant and anti-inflammatory activities. 4-PSQ improves cognitive impairment and depressive- and anxiety-like emotional abnormalities in mice by regulating the activity of Na+, K+-ATPase, the NFκB signaling pathway, and the expression of p21. 4-PSQ can be used for the research of neurological diseases.

CL 277082 is a potent and selective acyl CoA:cholesterol acyltransferase (ACAT) inhibitor in microsomes. CL 277082 inhibits ACAT with IC50 values of 0.14 μM for intestinal mucosal microsomes, 0.74 μM for liver, and 1.18 μM for rat adrenal. CL 277082 is a ACAT-catalyzed cholesterol esterification and cholesterol absorption inhibitor.

FR-182980 is an orally active ACAT1 inhibitor (IC50: 30 nM). FR-182980 has hypocholesterolemic activity and can be used for research of atherosclerosis.

CL-283796 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.

Bay-02752 (Bay o 2752) is a lipid-lowering agent. Bay-02752 inhibits acyl-CoA activity in liver microsomes (IC50 = 0.95 μg/mL). Bay-02752 inhibits intestinal cholesterol absorption in rats. Bay-02752 inhibits gallstone formation in hamsters.

Cs-2d is a selective ceramide synthases Cer1 inhibitor. Cs-2d has potent inhibitory activity toward C. neoformans Cer1, while maintaining a low off-target effect on human hCerS1. Cs-2d has potent antifungal activity with the significant growth inhibition. Cs-2d can be used for invasive fungal infections research.

CH-4630808 (sodium) is a serine palmitoyl transferase (SPT) inhibitor. CH-4630808 (sodium) exhibits anti-HCV activity.

SDZ-CPI-975 is a novel, reversible, and selective CPT I inhibitor. SDZ-CPI-975 effectively inhibits fatty acid oxidation and lowers blood glucose levels.

Obeversen sodium is an antisense oligonucleotide that inhibits the synthesis of Diacylglycerol acyltransferase 2 (DGAT-2). Obeversen sodium can be used in the research of nonalcoholic fatty liver disease.

Yakuchinone B is an Acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitor with hypocholesterolemic activity, which is found in the seeds of Zingiberaceae. Yakuchinone B inhibits rat hepatic ACAT with an IC50 value of 20.6 μM. Yakuchinone B is promising for research of hypercholesterolemia and atherosclerosis.

Epicochlioquinone A can inhibit rat liver microsomal ACAT with IC50 of 1.7 μM, inhibit plasma lecithin cholesterol acyltransferase (LCAT) with IC50 of 15.8 μM, and inhibit cholesterol absorption in rats by 50% at 75 mg/kg.

Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras.

ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD).

BAY 74-4113 is a DGAT1 inhibitor (IC50: 72 nM). BAY 74-4113 can be used in obesity research.

ALT-007 is an orally effective serine palmitoyltransferase (SPT) inhibitor. SPT is the rate-limiting enzyme for the de novo synthesis of ceramide. In a mouse model of age-related sarcopenia, ALT-007 can effectively restore the muscle mass and function impaired by aging. ALT-007 may enhance protein homeostasis in Caenorhabditis elegans and mouse models of aging and age-related diseases and play the role of a ceramide inhibitor.

BMS-963272 is a potent, selective MGAT2 inhibitor with IC50 of 7.1 nM/18 nM (hMGAT2/mMGAT2) and shows excellent efficacy, safety, and tolerability profile.

CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease.

2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines.

YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.

Amidepsine D is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.

Penicillide (Vermixocin A), isolated from Talaromyces derxii cultivated on rice, shows inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT).

Phenylpyropene A, a fungal metabolite, is a potent acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor with an IC50 of 0.8 μM.

Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).

Terpendole I, a fungal indoloditerpene, is a ACAT (acyl-CoA: cholesterol acyltransferase) inhibitor (IC50=145 µM).

VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia.

Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor (DGAT2i). Ervogastat alone reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Ervogastat combination with Clesacostat (an acetyl CoA-carboxylase inhibitor (ACCi)) can be used for the research of NASH with liver fibrosis therapy.