1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. MGAT2-IN-1

MGAT2-IN-1 

Cat. No.: HY-101857 Purity: 98.63%
Handling Instructions

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.

For research use only. We do not sell to patients.

MGAT2-IN-1 Chemical Structure

MGAT2-IN-1 Chemical Structure

CAS No. : 1800025-30-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 777 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2640 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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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.

IC50 & 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].

Molecular Weight

654.01

Formula

C₂₇H₂₁ClF₅N₇O₃S

CAS No.

1800025-30-2

SMILES

O=S(C1=CC2=C(N(C3=NC=C(C4=CC(C(F)(F)F)=NN4C)C=N3)CC2)C(N5C(CCC5)=O)=C1)(NC6=C(F)C=C(Cl)C=C6F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (191.13 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5290 mL 7.6451 mL 15.2903 mL
5 mM 0.3058 mL 1.5290 mL 3.0581 mL
10 mM 0.1529 mL 0.7645 mL 1.5290 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

MGAT2-IN-1AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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MGAT2-IN-1
Cat. No.:
HY-101857
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