Cas No.: | 1415559-41-9 |
Chemical Name: | 2H-Tetrazole-2-acetic acid, 5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-, 2,2,2-trifluoroacetate (1:1) |
Synonyms: | MK 8245 Trifluoroacetate; MK8245 Trifluoroacetate |
SMILES: | O=C(O)CN1N=NC(C2ON=C(N3CCC(OC4C(Br)=CC=C(F)C=4)CC3)C=2)=N1.FC(F)(F)C(=O)O |
Formula: | C19H17BrF4N6O6 |
M.Wt: | 581.2725 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | MK-8245 trifluoroacetate is a potent, selective liver-targeted stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 3, 3 and 1 nM for rat, mouse and human SCD1 enzyme, respectively; displays highly selective over the Δ-5 and Δ-6 desaturases (IC50>100 uM); has IC50 values of 68 nM and 1066 nM in Hum HepG2 and rat hepatocyte assays, demonstrates HepG2/hepatocyte ratio of 16:1; exhibits preclinical antidiabetic and antidyslipidemic efficacy in vivo, demonstrats maximal liver SCD inhibition while sparing inhibition in the skin and eye tissues associated with adverse events.DiabetesPhase 1 Discontinued |