2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. DGAT1-IN-4

DGAT1-IN-4 is a potent, orally active, and selective DGAT1 inhibitor with an IC50 of 17 nM. DGAT1-IN-4 exhibits >588-fold selectivity over DGAT2. DGAT1-IN-4 suppresses intracellular triglyceride synthesis in mouse myoblast cells. DGAT1-IN-4 suppresses body weight gain in diet-induced obese dogs. DGAT1-IN-4 can be used for the research of obesity.

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DGAT1-IN-4

DGAT1-IN-4 Chemical Structure

CAS No. : 1137671-16-9

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DGAT1-IN-4 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

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Description

DGAT1-IN-4 is a potent, orally active, and selective DGAT1 inhibitor with an IC50 of 17 nM. DGAT1-IN-4 exhibits >588-fold selectivity over DGAT2. DGAT1-IN-4 suppresses intracellular triglyceride synthesis in mouse myoblast cells. DGAT1-IN-4 suppresses body weight gain in diet-induced obese dogs. DGAT1-IN-4 can be used for the research of obesity[1].

IC50 & Target[1]

DGAT1

17 nM (IC50)

DGAT2

>10 μM (IC50)

In Vitro

DGAT1-IN-4 (compound 9) (2 h) inhibits intracellular triglyceride synthesis in C2C12 mouse myoblast cells with an IC50 of 151 nM[1].

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

DGAT1-IN-4 Related Antibodies
Parmacokinetics
Species Dose Route CL Vss T1/2 AUC0-t Cmax Tmax F
Rat[1] 1 mg/kg i.v. 9.5 mL/min/kg 0.6 L/kg 1.9 h 3857 nM·h / / /
Rat[1] 3 mg/kg p.o. / / / 10376 nM·h 3551 nM 1.2 h 90 %
In Vivo

DGAT1-IN-4 (compound 9) (1 mg/kg; i.g.; single dose) suppresses postprandial triglyceride excursions in dogs[1].
DGAT1-IN-4 (5 mg/kg; p.o.; daily; 21 days) reduces high-fat diet-induced body weight gain in dogs[1].

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

Animal Model: Beagle (male, 7-12 kg)[1]
Dosage: 1 mg/kg
Administration: i.g.; single dose
Result: Reduced the incremental area under the curve (AUC0-4ₕ) of plasma triglycerides.
Achieved a statistically significant reduction.
Animal Model: Beagle fed with a high fat diet[1]
Dosage: 5 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced body weight gain from 25% (vehicle group) to 11.7% over 21 days.
Lowered absolute body weight gain from 2.37 kg (vehicle group) to 1.1 kg.
Showed significant differences in body weight gain from day 13 onward.
Molecular Weight

496.57

Formula

C29H28N4O4
CAS No.
SMILES

O=C(O)C(C)(C)CC=1C=C(C(C2=NC=3C=CC(=CC3N2)C4=NN=C(O4)C=5C=CC(OC)=CC5)=C(C1)C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DGAT1-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DGAT1-IN-41137671-16-9AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferasediet-induced obesitySf9 insect cell membranesSalmonella typhimuriumC2C12 mouse myoblast cellspostprandial triglyceridesDGAT1DGAT2S9 metabolic activationdiet-induced obese dogsCaco-2 cellsInhibitorinhibitorinhibit

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