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 MkfGSpVv[3Srb36gZZN{[Xl? MmTMTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCGR1HUNUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTBwMEC3{txO MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDF6M{m0OEc,OThzOEO5OFQ9N2F-
Sf9 NIjIUINHfW6ldHnvckBie3OjeR?= NFLaSYc3OCCvaX7z MoTvTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDmeYxtKGynbnf0bEBpfW2jbjDES2FVOSCneIDy[ZN{\WRiaX6gV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yBzLEKt[Ill\WOjbn;5cE1{di2pbInj[ZJwdCCjczDzeYJ{fHKjdHWgZYZ1\XJiNkCgcYlveyCrbjDwdoV{\W6lZTDv[kBx[WyvaYTvfYwuOS1zNFOgZ49mdnq7bXWgRUBjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUCuNFA4QM7:TR?= MoHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5M{mxOVUoRjJ6N{O5NVU2RC:jPh?=
Sf9 NH\tXmRHfW6ldHnvckBie3OjeR?= Ml25NUBpeg>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJGRISVRzIHX4dJJme3OnZDDpckBU\jliY3XscJMh[XO|ZYPz[YQh[XNiZn;ycYF1cW:wIH;mJIRq\GWlYX7vfYxodHmlZYLvcEBxem:mdXP0JIFnfGW{IEGgbJIhfXOrbnegNVRENWSnY3Huc5ltNUOxQTDifUBj\XSjIIPjbY51cWyuYYTpc44h[2:3boTldkwhUUN3ME2wMlAz|ryP NEXl[mk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi2PFIzOCd-MkG4OlgzOjB:L3G+
Sf9 NFrnSFNHfW6ldHnvckBie3OjeR?= Mm[yTY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCGR1HUNUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTBwMEK0{txO MnvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThzOEO5OFQoRjF6MUizPVQ1RC:jPh?=
MA104 MUHBcpRqfmm{YXygZZN{[Xl? MU[yOEBpenN? M2Hu[WFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JHJwfGG4aYL1d{BUSTFzIHnuJG1COTB2IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44h[W[2ZYKgNlQhcHK|IHL5JIludXWwb3\seY9z\XOlZX70JIF{e2G7IHHu[EBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nzMEBGTDVyPUKzMlLPxE1? M2XlZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{[1OFEyLz5{MkO2OVQyOTxxYU6=
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

Solubility (25°C)

In vitro

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

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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