ABT-046

Cat. No.: HY-15197 Purity: 98.13%: FAQs
Data Sheet SDS COA Handling Instructions

ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC₅₀s of both 8 nM against human and mouse DGAT-1.

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

ABT-046 Chemical Structure

CAS No. : 1031336-60-3

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solution
10 mM * 1 mL in DMSO	USD 323	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 323	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 294	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 516	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2714	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC₅₀s of both 8 nM against human and mouse DGAT-1^[1].

IC₅₀ & Target

IC₅₀: 8 nM (hDGAT-1 and mDGAT-1)^[1]

In Vitro

ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC₅₀ of 78 nM^[1].
ABT-046 exhibits high in vitro permeability values in Caco-2 cells with no evidence of active efflux (efflux ratio = 1.4 and 1.1 at 0.5 and 5 μM, respectively)^[1].
ABT-046 demonstrates negligible turnover in microsome preparations from mouse and human livers^[1].

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

In Vivo

ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice^[1].
ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion in diet-induced obesity mice^[1].

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

Animal Model:	Male CD-1 mice, postprandial hyperlipidemia model^[1]
Dosage:	0.03, 0.3, or 3 mg/kg
Administration:	Oral gavage, single dose
Result:	Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C_2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively).

Animal Model:	Male C57BL/6J diet-induced obesity (DIO) mice^[1]
Dosage:	0.3 mg/kg
Administration:	Oral gavage, single dose
Result:	Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.

Animal Model:

CD-1 mice and Sprague-Dawley rats^[1]

Dosage:

10 mg/kg or 5 mg/kg

Administration:

Intravenous injection or oral gavage (Pharmacokinetic Analysis)

Result:

Selected Pharmacokinetic Properties of ABT-046^a^[1]

	mouse (10 mg/kg)	rat (5 mg/kg)
	iv^b
T_1/2 (h)	4.6	3.8
V_ss (L/kg)	0.3	0.3
Clp (L/h/kg)	0.1	0.05
	po^b
T_1/2 (h)	5.1	5.6
C_max (μg/mL)	17.4	9.3
AUC (μg h/mL)	151	130
F (%)	78	91

^a All values are mean values ± SEMs (n = 3 unless specified otherwise).
^b 1% Tween-80 in water.

Molecular Weight

350.41

Appearance

Solid

Formula

C₂₀H₂₂N₄O₂

CAS No.

1031336-60-3

SMILES

NC1=C(C2=CC=C([[email protected]]3CC[[email protected]](CC(O)=O)CC3)C=C2)C=NC4=CC=NN41

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 : 66.67 mg/mL (190.26 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8538 mL	14.2690 mL	28.5380 mL
5 mM	0.5708 mL	2.8538 mL	5.7076 mL
10 mM	0.2854 mL	1.4269 mL	2.8538 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (4.77 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 1.67 mg/mL (4.77 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 98.13%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (246 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Yeh VS, et al. Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of Acyl-CoA: Diacylglycerol acyltransferase 1. J Med Chem. 2012 Feb 23;55(4):1751-1757. [Content Brief]

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.

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

ABT-0461031336-60-3ABT046ABT 046AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT-1postprandial hyperlipidemiahigh in vitro permeabilityorally activeInhibitorinhibitorinhibit

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