DGAT1-IN-3

• CAT Number: I015032
• CAS Number: 939375-07-2
• Molecular Formula: C20H19F3N4O3
• Molecular Weight: 420.39
• Purity: ≥95%
• Synonyms: N-[6-[2-methoxyethyl(methyl)amino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide
• InChI: InChI=1S/C20H19F3N4O3/c1-27(10-11-29-2)15-9-8-14(12-24-15)25-18(28)16-17(20(21,22)23)30-19(26-16)13-6-4-3-5-7-13/h3-9,12H,10-11H2,1-2H3,(H,25,28)
• InChIKey: QEZWDFXCTTZZRI-UHFFFAOYSA-N
• SMILES: CN(CCOC)C1=NC=C(C=C1)NC(=O)C2=C(OC(=N2)C3=CC=CC=C3)C(F)(F)F

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].
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].
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 (Cmax) 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].

Reference

[1]. Gómez-Outes A, et al. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59.
 [Content Brief]

[2]. 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; 54(7): 2433-46.
 [Content Brief]

[3]. 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.