A922500

For research use only.

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

2 publications

A922500 Chemical Structure

CAS No. 959122-11-3

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.

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 MljXSpVv[3Srb36gZZN{[Xl? M1vNb2lvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiRFfBWFEh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD1yLkCwO:69VQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDF6M{m0OEc,OThzOEO5OFQ9N2F-
Sf9 MlnJSpVv[3Srb36gZZN{[Xl? NYHEdW0yPjBibXnudy=> M3LDdWlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSg[pVtdCCuZX7neIghcHWvYX6gSGdCXDFiZYjwdoV{e2WmIHnuJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiMTyyMYRq\GWlYX7vfYwue25vZ3z5Z4Vzd2xiYYOgd5Vje3S{YYTlJIFnfGW{IE[wJI1qdnNiaX6gdJJme2WwY3Wgc4YheGGubXn0c5ltNTFvMUTDJINw\W68eX3lJGEh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3ME2wMlAxPzkQvF2= Ml3CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5M{mxOVUoRjJ6N{O5NVU2RC:jPh?=
Sf9 NXnnXIxETnWwY4Tpc44h[XO|YYm= M1HaTVEhcHJ? NVP1XWVyUW6qaXLpeIlwdiCxZjDoeY1idiCGR1HUNUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IHHzd4V{e2WmIHHzJIZwem2jdHnvckBw\iCmaXTlZ4Fvd3muZ3z5Z4Vzd2xicILv[JVkfCCjZoTldkAyKGi{IIXzbY5oKDF2Qz3k[YNidm:7bD3Dc2Eh[nliYnX0ZUB{[2mwdHnscIF1cW:wIHPveY51\XJuIFnDOVA:OC5yMt88US=> NIf4eZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi2PFIzOCd-MkG4OlgzOjB:L3G+
Sf9 NXTSZ2NuTnWwY4Tpc44h[XO|YYm= NWjwUHRHUW6qaXLpeIlwdiCxZjDtc5V{\SC{ZXPvcYJqdmGwdDDES2FVOSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUCuNFI1|ryP NVTvWplRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUixPFM6PDRpPkG4NVg{QTR2PD;hQi=>
MA104 M2[wW2FvfGm4aYLhcEBie3OjeR?= MUmyOEBpenN? NF\ScmVCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBTd3SjdnnyeZMhW0FzMTDpckBOSTFyNDDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vKGGodHXyJFI1KGi{czDifUBqdW23bn;mcJVwemW|Y3XueEBie3OjeTDhcoQhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpd{whTUR3ME2yN{4z|ryP NX36TlNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzOlU1OTFpPkKyN|Y2PDFzPD;hQi=>

... 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

Animal Research:[1]
- Collapse
  • 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 powder
in solvent
Synonyms DGAT-1 Inhibitor 4a
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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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID