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MK-8245

Cat. No. M3518

MK-8245 Structure
Size Price Availability Quantity
5mg USD 210 In stock
10mg USD 300 In stock
50mg USD 820 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 467.25
Formula C17H16BrFN6O4
CAS Number 1030612-90-8
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MK-8245 supplier, Dehydrogenase, inhibitors

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