MK-8245

SKU: orb1305218

Description

MK-8245

Research Area

Metabolism Research

Key Properties

• CAS Number: 1030612-90-8
• MW: 467.25
• Purity: 98.18%
• Formula: C₁₇H₁₆BrFN₆O₄
• SMILES: OC(=O)Cn1nnc(n1)-c1cc(no1)N1CCC(CC1)Oc1cc(F)ccc1Br
• Target: Stearoyl-CoA Desaturase (SCD),Dehydrogenase
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:86 mg/mL (184.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.06 mM)

Bioactivity

• Target IC50:
  SCD1 (rat):3 nM|SCD1 (human):1 nM|SCD1 (mouse):3 nM
• In Vivo:
  In experiments conducted on rat liver cells exhibiting functional activity of OATPs, MK-8245 demonstrated a potent inhibitory effect on SCD, with an IC50 of 68 nM. However, in experiments with HepG2 cells, which lack active OATPs, the compound was less effective, showing an IC50 of 1 μM. In HepG experiments, MK-8245 displayed high selectivity towards Δ-5 and Δ-6 desaturases. MK-8245 contains a tetrazole acetic acid group, endowing it with the capability for OATP recognition and liver-targeting functions.
• In Vitro:
  In mice, rats, dogs, and cynomolgus monkeys, the primary site of action for MK-8245 (p.o.) is the liver, displaying minimal efficacy in tissues associated with potential adverse reactions. In eDIO mice, MK-8245 demonstrates a dose-dependent effect on glucose screening, enhancing glucose clearance (ED50: 7 mg/kg).

Storage & Handling

• Storage: store at low temperature,keep away from moisture,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, MK 8245, MK8245, MK-8245, StearoylCoADesaturase, StearoylCoADesaturase(SCD), SCD1 (human), SCD1 (mouse), SCD1 (rat), SCD, StearoylCoA Desaturase (SCD), Stearoyl-CoA Desaturase (SCD), Stearoyl-CoA Desaturase

Compound Identifiers

PubChem CID

24988881