Choose Your Country or Region

A922500

Name: A922500
Brand: Selleck Chemicals
SKU: S2674
Rating: 5 (5 reviews)

Synonyms: DGAT-1 Inhibitor 4a

Catalog No.S2674 Purity: 99.86%

A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

A922500 Chemical Structure

CAS: 959122-11-3

Selleck's A922500 has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.86%

99.86

Related compound libraries

Choose Selective Transferase Inhibitors

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
Sf9	Function assay		Inhibition of human recombinant DGAT1 expressed in Sf9 cells, IC50=0.007μM	18183944
Sf9	Function assay	60 mins	Inhibition of recombinant full length human DGAT1 expressed in Sf9 insect cells using 1,2-didecanoyl-sn-glycerol as substrate after 60 mins in presence of palmitoyl-1-14C coenzyme A by scintillation counting, IC50=0.0078μM	28739155
Sf9	Function assay	1 hr	Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scintillation counter, IC50=0.02μM	21868220
Sf9	Function assay		Inhibition of mouse recombinant DGAT1 expressed in Sf9 cells, IC50=0.024μM	18183944
MA104	Antiviral assay	24 hrs	Antiviral activity against Rotavirus SA11 in MA104 cells assessed as inhibition of viral replication after 24 hrs by immunofluorescent assay and Western blotting analysis, ED50=23.2μM	22365411
Click to View More Cell Line Experimental Data

Biological Activity

Description

Features

A potent, selective, and orally bioavailable DGAT-1 inhibitor.

Targets

human DGAT1 ^[1]	mouse DGAT1 ^[1]
7 nM	24 nM

In vitro
In vitro	A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. ^[1] A 922500 potently inhibits huDGAT-1 and mseDGAT-1. ^[2]
Kinase Assay	In vitro DGAT-1 activity inhibition assay
Kinase Assay	DGAT-1 activity is determined as follows: Assay buffer [20 mM HEPES (pH 7.5), 2 mM MgCl₂, 0.04% BSA] containing 50 μM of enzyme substrate (didecanoyl glycerol) and 7.5 μM radiolabeled acyl-CoA substrate. [1- ¹⁴ C]decanoyl-CoA) is added to each well of a phospholipid FlashPlate. A small aliquot of membrane (1 μg/well) is added to start the reaction, which is allowed to proceed for 60 minutes. The reaction is terminated upon the addition of an equal volume (100 μL) of isopropanol. The plates are sealed, incubated overnight and counted the next morning on a TopCount Scintillation Plate Reader. DGAT-1 catalyzes the transfer of the radiolabel-led decanoyl group onto the sn-3 position of didecanoyl glycerol. The resultant radiolabeled tridecanoyl glycerol (tricaprin) preferentially binds to the hydrophobic coating on the phospholipid FlashPlate. The proximity of the S15 radiolabeled product to the solid scintillant incorporated into the bottom of the FlashPlate induces fluor release from the scintillant, which is measured in the TopCount Plate Reader. Various concentrations (e.g. 0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1.0 μM, 10.0 μM) of A 922500 are added to individual wells prior to the addition of membranes. The potency of DGAT-1 inhibition for the A 922500 is determined by calculating the IC50 values defined as the inhibitor concentration from the sigmoidal dose response curve at which the enzyme activity is inhi

In Vivo
In vivo	Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. ^[1] A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. ^[2] A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. ^[3]
Animal Research	Animal Models	Thirteen-week-old male Golden Syrian hamsters with hyperlipidemia, Ten-week-old Male Zucker fatty rats
	Dosages	0.03, 0.3, and 3 mg/kg
	Administration	Oral gavage

References

Chemical lnformation & Solubility

Molecular Weight	428.48	Formula	C₂₆H₂₄N₂O₄
CAS No.	959122-11-3	SDF	Download A922500 SDF
Smiles	C1CC(C(C1)C(=O)O)C(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)NC(=O)NC4=CC=CC=C4
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 86 mg/mL ( (200.7 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	4.0mg/ml (9.34mM)	Taking the 1 mL working solution as an example, add 100 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	4.0mg/ml (9.34mM)	Taking the 1 mL working solution as an example, add 100 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.3mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL 86 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):