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Compound Overview
MK-8245 Trifluoroacetate (CAS 1415559-41-9) is a research-grade small molecule supplied by TargetMol.
Physical Properties
| CAS Number | 1415559-41-9 |
|---|---|
| Molecular Formula | C19H17BrF4N6O6 |
| Molecular Weight | 581.27 g/mol |
| SMILES | O=C(O)CN1N=NC(=N1)C=2ON=C(C2)N3CCC(OC4=CC(F)=CC=C4Br)CC3.O=C(O)C(F)(F)… |
| Form | Solid |
| Shipping | Room Temperature (RT) |
Biological Activity
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 uM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against delta-5 and delta-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.
Safety & Regulatory
For Research Use Only (RUO). Not for therapeutic, diagnostic, or clinical use. Wear appropriate PPE and consult the Safety Data Sheet (SDS) prior to handling.
When solubility is listed as < 1 mg/mL, the compound dissolves to less than 1 mg per milliliter in water at 25 °C, pH 7.4. Such compounds require an organic co-solvent such as DMSO to prepare a concentrated stock, which is then diluted into aqueous assay buffer. For cell-based assays, keep the final DMSO concentration below 0.1% (v/v) to avoid solvent-induced cytotoxicity.
Centrifuge the closed vial at 3000 rpm for 1–2 minutes to consolidate the powder at the bottom. For electrostatically charged powders, briefly warm the vial to room temperature and allow it to equilibrate before opening. Then add the appropriate solvent directly onto the powder and vortex before sonicating. Avoid tapping the vial vigorously, as this can generate fine powder aerosol.
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