1800025-30-2
1800025-30-2 structure
- Name: MGAT2-IN-1
- Chemical Name: MGAT2-IN-1
- CAS Number: 1800025-30-2
- Molecular Formula: C27H21ClF5N7O3S
- Molecular Weight: 654.01
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
- Create Date: 2018-04-24 10:54:49
- Modify Date: 2024-01-31 18:43:48
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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.
| Name | MGAT2-IN-1 |
|---|
| 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 |
| Molecular Formula | C27H21ClF5N7O3S |
|---|---|
| Molecular Weight | 654.01 |
| Storage condition | 2-8℃ |