BMS711939
BMS711939 is a selective agonist for peroxisome proliferator-activated receptor α (PPAR α), with EC50 of 4 nM and 4.5 μM, for human PPARα and human PPARγ. BMS711939 exhibits good pharmacokinetic characters in rats models. BMS711939 increases HDL cholesterol, reduces LDL cholesterol and triglycerides.
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- CAS. Nr.: 1000998-62-8
- Formel: C22H20ClFN2O6
- Molecular Weight:462.86
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
|
hPPARα 4 nM (IC50) |
hPPARγ 4.5 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
4 nM
Compound: 3; BMS-711939
|
Agonist activity at Gal4-tagged human PPAR-alpha expressed in HEK cells by transactivation assay
Agonist activity at Gal4-tagged human PPAR-alpha expressed in HEK cells by transactivation assay
|
[PMID: 27326332] |
| HEK293 | EC50 |
4511 nM
Compound: 3; BMS-711939
|
Agonist activity at Gal4-tagged human PPAR-gamma expressed in HEK cells by transactivation assay
Agonist activity at Gal4-tagged human PPAR-gamma expressed in HEK cells by transactivation assay
|
[PMID: 27326332] |
| HepG2 | EC50 |
>1.61 μM
Compound: 3; BMS-711939
|
Agonist activity at full length human PPAR-gamma transfected in human HepG2 cells by luciferase reporter gene assay
Agonist activity at full length human PPAR-gamma transfected in human HepG2 cells by luciferase reporter gene assay
|
[PMID: 27326332] |
| HepG2 | EC50 |
5 nM
Compound: 3; BMS-711939
|
Agonist activity at full length human PPAR-alpha transfected in human HepG2 cells by luciferase reporter gene assay
Agonist activity at full length human PPAR-alpha transfected in human HepG2 cells by luciferase reporter gene assay
|
[PMID: 27326332] |
Chemical Information
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CAS. Nr. 1000998-62-8
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Molecular Weight 462.86
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Formel C22H20ClFN2O6
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SMILES
O=C(CN(CC1=CC(OCC2=C(C)OC(C3=CC=C(Cl)C=C3)=N2)=CC=C1F)C(OC)=O)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)