Home Metabolism Transferase inhibitor - Acyltransferase inhibitor A922500

A922500

Catalog No.S2674 Synonyms: DGAT-1 Inhibitor 4a

For research use only.

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 No. 959122-11-3

Selleck's A922500 has been cited by 2 Publications

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Biological Activity

Description 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.
Features A potent, selective, and orally bioavailable DGAT-1 inhibitor.
Targets
human DGAT-1 [1]
()		 mouse DGAT-1 [1]
()
7 nM 24 nM
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 M3fuTmZ2dmO2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KESJQWSxJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:OC5yMEhOwG0> M2rtblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MUizPVQ1Lz5zOEG4N|k1PDxxYU6=
Sf9 MUDGeY5kfGmxbjDhd5NigQ>? MW[2NEBucW6| NWi3eGpIUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBnfWyuIHzlcod1cCCqdX3hckBFT0GWMTDlfJBz\XO|ZXSgbY4hW2Z7IHnud4VkfCClZXzsd{B2e2mwZzCxMFIu\GmmZXPhco96dC2|bj3ncJlk\XKxbDDhd{B{fWK|dILheIUh[W[2ZYKgOlAhdWmwczDpckBxemW|ZX7j[UBw\iCyYXztbZRwgWxvMT2xOGMh[2:nbor5cYUhSSCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwQVAvODB5ON88US=> M3fBcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{O5NVU2Lz5{OEezPVE2PTxxYU6=
Sf9 Mlv0SpVv[3Srb36gZZN{[Xl? MWSxJIhz NHiwUG1KdmirYnn0bY9vKG:oIHj1cYFvKESJQWSxJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNiYYPz[ZN{\WRiYYOg[o9zdWG2aX;uJI9nKGSrZHXjZY5wgWypbInj[ZJwdCCycn;keYN1KGGodHXyJFEhcHJidYPpcochOTSFLXTlZ4Fvd3muLVPvRUBjgSCkZYThJJNkcW62aXzsZZRqd25iY3;1cpRmeixiSVO1NF0xNjB{zszN M1fvUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOE[4NlIxLz5{MUi2PFIzODxxYU6=
Sf9 NGPGWVVHfW6ldHnvckBie3OjeR?= NFj0UpZKdmirYnn0bY9vKG:oIH3veZNmKHKnY3;tZolv[W62IFTHRXQyKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MD6wNlTPxE1? MkXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThzOEO5OFQoRjF6MUizPVQ1RC:jPh?=
MA104 MYDBcpRqfmm{YXygZZN{[Xl? M{HyT|I1KGi{cx?= MnrxRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgVo91[X[rcoXzJHNCOTFiaX6gUWEyODRiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjCyOEBpenNiYomgbY1ufW6xZnz1c5Jme2OnboSgZZN{[XliYX7kJHdme3Sncn6gZoxwfHSrbnegZY5idHm|aYOsJGVFPTB;MkOuNu69VQ>? MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN4NUSxNUc,OjJ|NkW0NVE9N2F-
Click to View More Cell Line Experimental Data
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]

Protocol (from reference)

Animal Research:[1]
  • 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
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 86 mg/mL
(200.7 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.

 20mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 428.48
Formula

C26H24N2O4
CAS No. 959122-11-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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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.
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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.

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