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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.

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].

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

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

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.

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

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.

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

Amitivir (LY 217896) is an inosine monophosphate dehydrogenase inhibitor. Amitivir inhibits the replication of dividing MDCK cells. Amitivir was associated with asymptomatic rises in serum uric acid levels and was ineffective in modifying the virologic or clinical course of experimental influenza A (H1N1) virus infection.

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

dWIZ-1 ((rac)-dWIZ-1) is a potent WIZ molecular gel degrader that recruits WIZ (ZF7) to the cereblon thereby inducing degradation and thus induction of haemoglobin fetalis (HbF) in erythroblasts, which can be used to study sickle cell disease (SCD).

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.

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.

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019). SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg/kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

Vibozilimod (SCD-044) is S1P receptor-1 (S1PR1) agonist .

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.

LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, targeting LXRβ (IC50: 0.36 μM) and LXRα (IC50: 2.25 μM). It serves as an adipogenesis inhibitor, downregulating LXR target genes SREBP-1c, ACC, FAS, and SCD-1, and demonstrates hypolipidemic activity in Triton WR-1339-induced hyperlipidemic mice.

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.