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BioAssay: AID 662546

Transactivation of human PPARalpha expressed in african green monkey CV1 cells at 30 uM by luciferase reporter gene assay relative to Wy14643

Amorphastilbol (APH-1), isolated from a Robinia pseudoacacia var. umbraculifer [corrected] seed extract, is a biologically interesting natural trans-stilbene compound with dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist activity. After total synthesis of APH-1 and its derivatives by Pd-catalyzed Suzuki-Miyaura cross-coupling of a common (E)-styryl bromide intermediate more ..
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Inconclusive(5)
 
 
Unspecified(7)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Inconclusive(5)
 
 
Unspecified(7)
 
 
 Related BioAssays
 Related BioAssays
AID: 662546
Data Source: ChEMBL (819635)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Peroxisome proliferator-activated receptor alpha; Short=PPAR-alpha; AltName: Full=Nuclear receptor subfamily 1 group C member 1
Description ..   
Protein Family: The ligand binding domain of peroxisome proliferator-activated receptors
Comment ..   

Gene:PPARA     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Total synthesis and dual PPARalpha/gamma agonist effects of amorphastilbol and its synthetic derivatives.

Abstract: Amorphastilbol (APH-1), isolated from a Robinia pseudoacacia var. umbraculifer [corrected] seed extract, is a biologically interesting natural trans-stilbene compound with dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist activity. After total synthesis of APH-1 and its derivatives by Pd-catalyzed Suzuki-Miyaura cross-coupling of a common (E)-styryl bromide intermediate and various aromatic trifluoroborate compounds, we biologically evaluated APH-2-APH-12 for PPAR agonist activity. APH-4 and APH-11 were effective PPARalpha/gamma transcriptional activators, compared with APH-1. Therefore, we suggest that APH-4 and APH-11 are novel dual PPARalpha/gamma agonists and are potentially useful for treating type 2 diabetes by enhancing glucose and lipid metabolism.
(PMID: 22579420)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Test Type: In vitro
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Emax activity commentEmax activity commentString
2Emax standard flagEmax standard flagInteger
3Emax qualifierEmax qualifierString
4Emax published valueEmax published valueFloat%
5Emax standard valueEmax standard valueFloat%

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
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