Stearoyl-CoA Desaturase (SCD)

GSK1940029 (SCD inhibitor 1) is an inhibitor of stearoyl-CoA desaturase (SCD).

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].

SW209049 is a stearoyl-CoA 9-desaturase inhibitor. SW209049 exhivits potent activity against H2122 cell with IC50 of 0.13uM.

Elemicin (Elemicine) is a constituent of several plant species' essential oils with anticholinergic effects in human.

Sesamin is a selective delta 5 desaturase inhibitor in the biosynthesis of polyunsaturated fatty acids and is a lignan abundantly present in sesame oil. It has potent neuroprotective effects against cerebral ischemia.

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

SLC13A5-IN-1 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5) that completely blocks the uptake of 14C-citrate, with an IC50 of 0.022 μM in HepG2 cells.

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

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.

MK-8245 analog is an analog of MK-8245 which is a liver-targeted Inhibitor of Stearoyl-CoA Desaturase (SCD). It is useful for the Treatment of Dyslipidemia and Diabetes.

FASN/SCD-IN-1 is a Silybin derivative and an orally active inhibitor of fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD). In vitro, FASN/SCD-IN-1 demonstrates the ability to inhibit lipid deposition, reduce the transcription levels of FASN and SCD, and exhibits antioxidant, anti-inflammatory, and antifibrotic activities. It shows significant hepatoprotective effects in rat models of acute liver injury and improves pathological features such as steatosis, inflammation, and fibrosis in a mouse model of myeloproliferative-associated steatohepatitis (MASH). FASN/SCD-IN-1 can be used for MASH research.

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.

CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).

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].

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

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

SC-26196 is an orally active inhibitor of Delta6 desaturase (D6D) with IC50 of 0.2 µM in a rat liver microsomal assay, with antiinflammatory properties.

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

T-3764518 is a novel and potent inhibitor of stearoyl coenzyme A desaturase (SCD) with an IC50 of 4.7 nM.

D5D-IN-326 is an orally active delta-5 desaturase (D5D) inhibitor (IC50s: 72 and 22 nM for rat and human D5D in enzymic and cell-based assays). It has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in die