Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM[1].
A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.
T-3764518 is a novel and potent stearoyl coenzyme A desaturase (SCD) inhibitor with an IC50 of 4.7 nM.
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses.
SCD inhibitor 1 is a stearoyl-coa desaturase (SCD) extracted from patent WO/2009060053 A1, compound example 16.
PluriSln 1 is an inhibitor of stearoyl-coA desaturase (SCD), and is a pluripotent cell-specific inhibitor.
SSI-4 is an inhibitor of Stearoyl CoA desaturase 1 (SCD1) , which can be modified with 11C, used as a ligand to in vivo small animal PET/CT imaging of SCD1[1].
MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.IC50 value: 1 nM (hSCD1) [1]Target: SCD1in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1].in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg.
CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.
MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an EC50 of 2.3 nM for rSCD1[1].
SCD1 inhibitor-4 is a potent, orally active stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes[1].
YTX-465 (YTX465) is a specific small molecule that rescues yeast from a-Syn cytotoxicity with EC50 of 15 nM, via inhibiting Ole1, the yeast homolog of human stearoyl-CoA desaturase (SCD); YTX-465 is inactive at SCD1.
XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.
SCD1-IN-1 is a SCD1 inhibitor (IC50: 5.8 nM). SCD1-IN-1 can be used in the research of dermatologic condition[1].
SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer[1].
CAY10566 is a stearoyl-CoA desaturase (SCD) inhibitor.
SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor[1].
SCD1/5-IN-1 (Compound 10) is a SCD1/5 inhibitor. SCD1/5-IN-1 can be used for research of neurological disease[1].
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer[1].
Elemicin is a alkenylbenzene widely distributed in many herbs and spices. Elemicin inhibits Stearoyl-CoA Desaturase 1 (SCD1) by metabolic activation. Elemicin is one of the main components in aromatic food and has antimicrobial, antioxidant, and antiviral activities. Elemicin possesses genotoxicity and carcinogenicity[1].
MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.IC50 value: 1 nM (hSCD1) [1]Target: SCD1in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1].in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg.