MGAT2-IN-1
Names
[ CAS No. ]:
1800025-30-2
[ Name ]:
MGAT2-IN-1
Biological Activity
[Description]:
MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
[Related Catalog]:
[Target]
IC50: 7.8 nM (Human MGAT2), 2.4 nM (Mouse MGAT2)[1]
[In Vivo]
MGAT2-IN-1 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG AUC in mice. MGAT2-IN-1 does not decrease MG absorption but inhibits MGAT2-dependent TG/DG resynthesis. In the lipid utilization analysis, MGAT2-IN-1 significantly increases free fatty acid (FFA) and acylcarnitine levels. MGAT2-IN-1 (30 mg/kg) also significantly reduces food intake dose dependently, suppresses BW gains. MGAT2-IN-1 shows anti-diabetic effects in mice[1].
[Animal admin]
Mice: Overnight-fasted mice undergo MTT in the morning. First, they are orally administered vehicle (0.5% methylcellulose solution) or MGAT2-IN-1 suspended in 0.5% methylcellulose. Six or 16 h after dosing, they are intraperitoneally injected 500 mg/kg Pluronic F-127 to inhibit plasma TG hydrolysis by lipoprotein lipase (LPL). Thirty minutes after injection, the mice are given an oral liquid meal (10 mL/kg) comprising an admixture of corn oil and Ensure-H (3:17 v/v). Blood samples are collected at 0, 2 and 4 h after oral gavage of the liquid meal. Area under the curve (AUC) of chylomicron TG (CM/TG), which is synthesised from dietary fat in the small intestine, is calculated by subtracting plasma TG levels of a liquid meal-untreated group from plasma TG levels of each treated group.
[References]
[Related Small Molecules]
Avasimibe
|
LCQ-908
|
DGAT-3
|
A922500
|
Xanthohumol
|
PF-04620110
|
AZD7687
|
DGAT-1 inhibitor 2
|
DGAT1-IN-1
|
K-604 dihydrochloride
|
PF-06471553
|
YM17E
|
ABT-046
|
RP 70676
|
Furan-2-carboxylic acid
Chemical & Physical Properties
[ Molecular Formula ]:
C27H21ClF5N7O3S
[ Molecular Weight ]:
654.01
[ Storage condition ]:
2-8℃