MK-8245 Trifluoroacetate - CAS 1415559-41-9

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 μM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against Δ-5 and Δ-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.

Others, Stearoyl-CoA Desaturase (SCD)

Metabolism, Others

1415509

C19H17BrF4N6O6

581.27

OC(=O)C(F)(F)F.OC(=O)Cn1nnc(n1)-c1cc(no1)N1CCC(CC1)Oc1cc(F)ccc1Br

-20°C

Ice Packs

Small Compound