1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. DGAT1-IN-3

DGAT1-IN-3 

Cat. No.: HY-16434
Handling Instructions

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.

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

DGAT1-IN-3 Chemical Structure

DGAT1-IN-3 Chemical Structure

CAS No. : 939375-07-2

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Description

DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC50s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome[1][2].

IC50 & Target

IC50: 38 nM (human DGAT-1); 120 nM (rat DGAT-1)[2]

In Vitro

DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM[1].
DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC50 of 0.66 μM[1].

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 (Cmax) 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].

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: Cmax (24 μM); T1/2 (1.95 h).
Molecular Weight

420.39

Formula

C₂₀H₁₉F₃N₄O₃

CAS No.

939375-07-2

SMILES

O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (237.87 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DGAT1-IN-3AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT-1obesitydyslipidemiametabolicsyndromeInhibitorinhibitorinhibit

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Product Name:
DGAT1-IN-3
Cat. No.:
HY-16434
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