DGAT1-IN-3 

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. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome^[1][2].

IC50: 38 nM (human DGAT-1); 120 nM (rat DGAT-1)^[2]

DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC₂₀ of 0.2 μM^[1].
DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC₅₀ of 0.66 μM^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile^[2].
DGAT1-IN-3 (50 mg/kg; p.o) exhibits good oral bioavailability (77%) and the maximum exposure level in plasma (C_max) is 24 μM^[2].
DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

420.39

Solid

C₂₀H₁₉F₃N₄O₃

939375-07-2

O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Yimin Q, et, al. Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem. 2011 Apr 14;  [Content Brief]

  [2]. Weiya Y, et, al. Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors. Bioorg Med Chem Lett. 2011 Dec 1; 21(23): 7205-9.