1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMGAT2-IN-1Cat. No.: HY-101857CAS No.: 1800025-30-2分式: CHClFNOS分量: 654.01作靶點: Acyltransferase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (191.13 m

2、M)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.5290 mL 7.6451 mL 15.2903 mL5 mM 0.3058 mL 1.5290 mL 3.0581 mL10 mM 0.1529 mL 0.7645 mL 1.5290 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MGAT2-IN-1種可服的單酰油酰 轉(zhuǎn)移酶 (MGAT2) 抑制劑，對和 MGA

3、T2 的 IC50 值分別為 7.8和 2.4 nM。IC50 & Target IC50: 7.8 nM (Human MGAT2), 2.4 nM (Mouse MGAT2) 1體內(nèi)研究MGAT2-IN-1 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEAUC in mice. MGAT2-IN-1 does not decrease MG absorption but

4、inhibits MGAT2-dependent TG/DGresynthesis. In the lipid utilization analysis, MGAT2-IN-1 significantly increases free fatty acid (FFA) andacylcarnitine 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

5、 mice 1.PROTOCOLAnimal Mice: Overnight-fasted mice undergo MTT in the morning. First, they are orally administered vehicle (0.5%Administration 1 methylcellulose solution) or MGAT2-IN-1 suspended in 0.5% methylcellulose. Six or 16 h after dosing, theyare intraperitoneally injected 500 mg/kg Pluronic

6、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 anadmixture of corn oil and Ensure-H (3:17 v/v). Blood samples are collected at 0, 2 and 4 h after oral gavageof the liquid meal. Area under

7、the curve (AUC) of chylomicron TG (CM/TG), which is synthesised from dietaryfat in the small intestine, is calculated by subtracting plasma TG levels of a liquid meal-untreated group fromplasma TG levels of each treated group.MCE has not independently confirmed the accuracy of these methods. They ar

8、e for reference only.REFERENCES1. Take K, et al. Pharmacological Inhibition of Monoacylglycerol O-Acyltransferase 2 Improves Hyperlipidemia, Obesity, and Diabetes byChange in Intestinal Fat Utilization. PLoS One. 2016 Mar 3;11(3):e0150976.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo