RO-5006036

Product NameRO-5006036
CAS939375-07-2
MFC20H19F3N4O3
MW420.39
EINECS
MOL File939375-07-2.mol

Chemical Properties

form	Solid
color	Light yellow to yellow

Usage And Synthesis

Description

RO-5006036, also known as DGAT1-IN-3, is a potent, selective and orally bioavailable inhibitor of DGAT-1

Uses

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].

in vivo

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].

Animal Model:	Three-month-old male Sprague Dawley DIO rats (fed with a high-fat diet)^[2]
Dosage:	0, 5, 25, 50 mg/kg; once daily for three weeks
Administration:	P.o. administration
Result:	Reduced cumulative body weight gain in a dose-dependent manner and was well tolerated in rats.

Animal Model:	Male Wistar rats^[2]
Dosage:	50 mg/kg for p.o. and 5 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:	P.o. and i.v. administration
Result:	C_max (24 μM); T_1/2 (1.95 h).

References

[1] Gómez-Outes A, et al. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59. DOI:10.1177/1753944710387808
[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. DOI:10.1021/jm101580m
[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.

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