Medchemexpress LLC DGAT1-IN-3 | 939375-07-2 | 99.9% | 420.39 | 50 MG

Supplier:  Medchemexpress LLC HY1643450MG

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. It could be used to research of obesity, dyslipidemia, and metabolic syndrome.

• IC50 of 38 nM for human DGAT-1; 120 nM for rat DGAT-1
• Inhibits human DGAT1 expressed in CHOK1 cells with an EC50 of 0.66 μM
• Blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM
• Reduces weight gain and plasma triglycerides, and improves lipid profile (5-50 mg/kg; p.o once daily for three weeks)
• Exhibits good oral bioavailability (77%) and a maximum exposure level in plasma (Cmax) of 24 μM (50 mg/kg; p.o)
• Exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg) (5 mg/kg; i.v)

Catalog No. 50-003-94474