7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one
7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one is a dual agonist of PPARα and PPARγ, with an EC50 of 23.10 μM for human PPARα and an EC50 of 22.29 μM for human PPARγ. 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one regulates the expression of lipid metabolism-related genes via PPARα, and modulates the expression of genes associated with glucose homeostasis and adipogenesis via PPARγ. 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one can be used in the research of type 2 diabetes and metabolic syndrome.
For research use only. We do not sell to patients.
- CAS No.: 139256-06-7
- Formula: C16H12O4
- Molecular Weight:268.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PPARα 23.10 μM (EC50) |
PPARγ 22.29 μM (EC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
22.29 μM
|
Activation of PPARγ in human embryonic kidney HEK 293 cells assessed via luciferase reporter gene assay with 48 h incubation, normalized to β-galactosidase signal.
Activation of PPARγ in human embryonic kidney HEK 293 cells assessed via luciferase reporter gene assay with 48 h incubation, normalized to β-galactosidase signal.
|
jm900964r |
| HEK293 | EC50 |
12.44 μM
Compound: 9
|
Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
|
[PMID: 23265844] |
| HEK293 | EC50 |
22.29 μM
Compound: 9
|
Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
|
[PMID: 23265844] |
| HEK293 | EC50 |
23.10 μM
|
Activation of PPARα in human embryonic kidney HEK 293 cells assessed via luciferase reporter gene assay with 48 h incubation, normalized to β-galactosidase signal.
Activation of PPARα in human embryonic kidney HEK 293 cells assessed via luciferase reporter gene assay with 48 h incubation, normalized to β-galactosidase signal.
|
jm900964r |
| HEK293 | EC50 |
33.13 μM
Compound: 9
|
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
|
[PMID: 23265844] |
In Vitro
7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one (compound 76) (48 h) potently activates PPARγ in HEK 293 cells with an EC50 of 22.29 μM; it also potently activates PPARα with an EC50 of 23.10 μM[1].
7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one (10-100 μM; 48 h) exhibits low cytotoxicity in HEK 293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 139256-06-7
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Molecular Weight 268.26
-
Formula C16H12O4
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SMILES
COC1=CC=CC(=C1)C2=COC3=C(C2=O)C=CC(=C3)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one
- 139256-06-7
- PPAR
- metabolic syndrome
- type II diabetes mellitus
- PPARγ
- glucose homeostasis-related gene expression
- human embryonic kidney cells
- PPARα
- human PPARα
- human PPARγ
- lipid metabolism-related gene expression
- adipogenesis-related gene expression
- Inhibitor
- inhibitor
- inhibit