[CAS NO. 939375-07-2] DGAT1-IN-3
PRODUCTS SPECIFICATIONS [939375-07-2]
DESCRIPTION [939375-07-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 420.39 |
| Molecular Formula | C20H19F3N4O3 |
| SMILES | O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3 |
Summary
IC50 & Target
IC50: 38 nM (human DGAT-1); 120 nM (rat DGAT-1) [2]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL ( 237.87 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3787 mL | 11.8937 mL | 23.7874 mL |
| 5 mM | 0.4757 mL | 2.3787 mL | 4.7575 mL |
| 10 mM | 0.2379 mL | 1.1894 mL | 2.3787 mL |
-
1.
References
- [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;
- [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.