scd1

SCD1 inhibitor-4 is stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.

SCD1 inhibitor-1 is a potent, liver-selective inhibitor of stearoyl-CoA desaturase-1 (SCD1).

SCD1 inhibitor-3 (ML-270) is a highly effective and orally available compound that inhibits SCD1 with remarkable safety. SCD1 inhibitor-3 demonstrates strong potential for research in metabolic diseases, including obesity, type II diabetes, and dyslipidemia, as well as various skin conditions like acne and cancer.

XEN723 is a potent thiazolylimidazolidinone Stearoyl-CoA Desaturase (SCD1) inhibitor(IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively).

CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl

CVT-11127 is an StearoylCoA Desaturase-1 (SCD1) inhibitor.

SCD1-IN-1, a potent inhibitor of SCD1 (IC50: 5.8 nM), is valuable in dermatologic research [1].

SCD1 Inhibitor is a novel stearoyl-CoA desaturase1 (SCD1) inhibitor.

SCD1/5-IN-1 (Compound 10), a selective SCD1/5 inhibitor, is utilized in the research of neurological diseases [1].

Sterculic acid, a stearoyl-CoA desaturase-1 (SCD1) inhibitor, effectively suppresses delta-9 desaturase (Δ9D) activity in a dose-dependent manner, exhibiting an inhibition concentration (IC50) value of 0.9 μM [1].

MF-438 is an effective and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor (EC50: 2.3 nM for rSCD1).

PluriSIn 1 (NSC 14613) is an inhibitor of stearoyl-CoA desaturase (SCD1), the key enzyme in oleic acid biosynthesis, highlighting a unique role for lipid metabolism in hPSCs.

PFM046 is an antagonist of the liver X receptor (LXR), effectively inhibiting the activation of LXRα and LXRβ, with IC50 values of 2.04 μM and 1.58 μM respectively. It reduces the expression of SCD1 and FASN while increasing ABCA1 expression, and demonstrates antitumor activity in mouse models.

MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function.

MK-8245 trifluoroacetate is a phenoxy piperidine isoxazole derivative functioning as a potent, liver-targeting stearoyl-CoA desaturase (SCD) inhibitor, demonstrating significant anti-diabetic and anti-dyslipidemic effects. It showcases high specificity and efficacy against SCD1 across various species, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1. MK-8245's mechanism includes a tetrazole acetic acid moiety that facilitates liver-targeting through OATPs recognition. Its inhibition potency in rat hepatocyte assays (IC50 of 68 nM) surpasses that in HepG2 cell assays devoid of active OATPs (IC50 of ~1 μM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against Δ-5 and Δ-6 desaturases in comparative assays. In vivo studies reveal MK-8245's preferential liver distribution in mice, rats, dogs, and rhesus monkeys, underscoring its potential for minimizing adverse effects in non-target tissues. Additionally, its administration in eDIO mice before glucose challenges significantly improves glucose clearance, indicating its therapeutic promise in diabetes management.

A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.

Aramchol (C20-FABAC), also known as arachidyl amido cholanoic acid, is a conjugate of arachidic acid and cholic acid. It reduces ex vivo cholesterol crystallization in native human bile and dissolves pre-formed cholesterol crystals in a dose-dependent manner.

SSI-4 is a Stearoyl CoA desaturase 1 (SCD1) inhibitor that can be labeled with carbon-11 (11C) for use as a ligand in small animal in vivo PET/CT imaging studies of SCD1 [1].

YTX-465 is an inhibitor of both stearoyl-CoA desaturase(IC50s = 39 nM) and Ole1 (IC50s = 30.4 μM).

Agrimonolide, a compound derived from isocoumarins and found mainly in the herb Agrimonia pilosa Ledeb, has significant biological activity. agrimonolide exerts anti-inflammatory effects by inhibiting lipopolysaccharide (LPS)-induced activation of JAK-STATs and p38 MAPKs signaling pathways. Agrimonolide and its derivative, desmethyl agonolide, have been shown to be effective in increasing insulin-mediated glycogen levels in hepatocytes and may play a key role in regulating insulin-resistant HepG2 cells. agrimonolide exhibits inhibitory effects on cancer progression and induction of cell death and apoptosis by targeting SCD1 in ovarian cancer cells. In particular, Agrimonolide exhibited a dose-dependent inhibition of proliferation, migration and invasion of A2780 and SKOV-3 cells, while promoting apoptosis. The compound was also found to induce iron-mediated cell death while increasing reactive oxygen species (ROS) and total iron levels.Agrimonolide readily crosses the blood-brain barrier, suggesting its potential for therapeutic applications in neurological disorders.