GW 9578
Based on 1 publication(s) in Google Scholar
GW9578 is a subtype-selective PPARα agonist (EC50s of 5 and 50 nM for murine and human PPAR-α) with potent lipid-lowering activity.
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- Reinheit: 99.6%
- CAS. Nr.: 247923-29-1
- Formel: C26H34F2N2O3S
- Molecular Weight:492.62
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Speicherung:
Solution, -20°C, 2 years
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) GW 9578
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Biologische Aktivität
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mouse PPARα 5 nM (EC50) |
h-PPARα 50 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
0.005 μM
Compound: 8
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Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells
Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
0.05 μM
Compound: 8
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Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
1 μM
Compound: 8
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Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
1.4 μM
Compound: 8
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Compound was tested for agonist activity on human Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
Compound was tested for agonist activity on human Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
1.5 μM
Compound: 8
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Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
2.6 μM
Compound: 8
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Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells
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[PMID: 10508427] |
| CV-1 | EC50 |
0.05 μM
Compound: GW-9578
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In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR alpha ligand binding domain
In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR alpha ligand binding domain
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[PMID: 11354382] |
| CV-1 | EC50 |
1 μM
Compound: GW-9578
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In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR gamma ligand binding domain
In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR gamma ligand binding domain
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[PMID: 11354382] |
| CV-1 | EC50 |
1.4 μM
Compound: GW-9578
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In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR delta ligand binding domain
In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR delta ligand binding domain
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[PMID: 11354382] |
| HEK293 | EC50 |
0.15 μM
Compound: GSK-9578
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Agonist activity at PPARdelta expressed in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARdelta expressed in HEK293 cells by GAL4 transactivation assay
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[PMID: 18029176] |
| HEK293 | EC50 |
0.45 μM
Compound: GSK-9578
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Agonist activity at PPARalpha expressed in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARalpha expressed in HEK293 cells by GAL4 transactivation assay
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[PMID: 18029176] |
| HEK293 | EC50 |
0.5 μM
Compound: GSK-9578
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Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay
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[PMID: 18029176] |
| HeLa | EC50 |
250 nM
Compound: 26, GW-9578
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Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
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[PMID: 19275963] |
| HeLa | EC50 |
250 nM
Compound: 26, GW-9578
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Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
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[PMID: 19275963] |
| HeLa | EC50 |
1 μM
Compound: 26, GW-9578
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Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
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[PMID: 19275963] |
| HepG2 | EC50 |
78 nM
Compound: gw9578
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Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
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[PMID: 17157019] |
GW9578 exhibits activities on Murine PPAR-α, PPAR-γ, and PPAR-δ with EC50s of 0.005, 1.5, 2.6 μm, respectively. GW9578 exhibits activities on Human PPAR-α, PPAR-γ, and PPAR-δ with EC50s of 0.05, 1, and 1.4 μm, respectively[2].
Treatment of the CD8+ T-cell line, TK.1 cells with GW9578 (10 nM-1 μM; for 24 hours) is able to induce a dose-dependent increase in the amount of relative luciferase activity[3].
Treatment of murine T-cell thymoma EL-4 T cells with GW9578 (10 nM-10 μM; for 2 hours) leads to a significant decrease in IL-2 production compared with control cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 247923-29-1
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Appearance Liquid
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Molecular Weight 492.62
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Formel C26H34F2N2O3S
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Color Colorless to light yellow
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SMILES
CC(C)(SC1=CC=C(CCN(C(NC2=CC=C(F)C=C2F)=O)CCCCCCC)C=C1)C(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Solution, -20°C, 2 years
Publications (1)
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Journal Impact Factor
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Most Recent
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Islets
Annexin A1 exacerbates islet stellate cell activation by regulating triglyceride catabolism via the PPARα/ACOX1/CYP4a pathway. [Abstract]2026 Dec 31;18(1):2633793. PMID: 41723748
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. P J Brown, et al. A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity. J Med Chem. 1999 Sep 23;42(19):3785-8. [Content Brief]
[2]. Alexandre Trifilieff, et al. PPAR-alpha and -gamma but not -delta agonists inhibit airway inflammation in a murine model of asthma: in vitro evidence for an NF-kappaB-independent effect. Br J Pharmacol. 2003 May;139(1):163-71. [Content Brief]
[3]. Dallas C Jones, et al. Nuclear receptor peroxisome proliferator-activated receptor alpha (PPARalpha) is expressed in resting murine lymphocytes. The PPARalpha in T and B lymphocytes is both transactivation and transrepression competent. J Biol Chem. 2002 [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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