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MK-8245 is a highly potent liver-targeted stearoyl-CoA desaturase (SCD) inhibitor with an IC50 of 1 nM for human SCD1 enzyme. MK-8245 inhibits the SCD enzyme solely in the liver and not in other tissues for the following reasons. When SCD inhibition has been measured by desaturation index in tissues of rodents treated with MK-8245, the desaturation index is significantly decreased in liver but not in other tissues such as skin, eye and adipose tissue. MK-8245 is distributed primarily to the liver, with low exposure in tissues associated with potential adverse events. MK-8245 is significantly shifted in the non-OATP HepG2 cellular assay. MK-8245 should possess the desired lack of cell penetration. MK-8245 ameliorates glucose clearance dose-dependently to a similar extent with an ED50 of 7 mg/kg.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male C57/Bl6 mice |
| Formulation | Suspended in 1% methocel in saline |
| Dosages | ~30 mg/kg |
| Administration | Orally |
| Molecular Weight | 467.25 |
| Formula | C17H16BrFN6O4 |
| CAS Number | 1030612-90-8 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Takayuki Hishiki, et al. Stearoyl-CoA desaturase-1 is required for flavivirus RNA replication
| Related Stearoyl-CoA Desaturase Products |
|---|
| Aramchol
Aramchol is a novel fatty acid bile acid coupling agent with oral activity and an inhibitor of SCD1, which acts by inhibiting SCD1 expression in hepatocytes and hepatic astrocytes, and can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| CVT-12012
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. |
| CAY10566
CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 blocks 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) |
| GSK1940029
GSK1940029 (SCD inhibitor 1) is a potent acyl-CoA desaturase (SCD) inhibitor. |
| A939572
A939572 is a potent, orally active stearyl CoA desaturase 1 SCD1 inhibitor that acts on mSCD1 and hSCD1 with IC50 <4 nM and 37 nM, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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