| Identification | Back Directory | [Name]
RO-5006036 | [CAS]
939375-07-2 | [Synonyms]
RO-5006036
DGAT1-IN-3
4-Oxazolecarboxamide, N-[6-[(2-methoxyethyl)methylamino]-3-pyridinyl]-2-phenyl-5-(trifluoromethyl)-
N-[6-[2-methoxyethyl(methyl)amino]pyridin-3-yl]-2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carboxamide | [Molecular Formula]
C20H19F3N4O3 | [MOL File]
939375-07-2.mol | [Molecular Weight]
420.39 |
| Hazard Information | Back Directory | [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 (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]. | 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: | Cmax (24 μM); T1/2 (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. |
|
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
|