NS-220
NS-220 is an orally active PPARα agonist with high subtype selectivity, with EC50 values of 1.9×10-8 M, 9.6×10-6 M and >10-4 M for PPARα, PPAR γ and PPARδ, respectively. NS-220 is used in the research for hyperlipidemia or metabolic disorders in type-2 diabetes.
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- CAS No.: 377731-45-8
- Formule: C21H27NO5
- Masse moléculaire:373.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PPARα 19 nM (EC50) |
PPARγ 9.6 μM (EC50) |
PPARδ >1 mM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
>100 μM
Compound: 14d, NS-220
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Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| CV-1 | EC50 |
0.01 μM
Compound: 14d, NS-220
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Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| CV-1 | EC50 |
0.03 μM
Compound: 14d, NS-220
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Agonist activity at mouse PPARalpha expressed in CV1 cells by transactivation assay
Agonist activity at mouse PPARalpha expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| CV-1 | EC50 |
9.6 μM
Compound: 14d, NS-220
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Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
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[PMID: 17964792] |
| HepG2 | EC50 |
0.052 μM
Compound: NS-220
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Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells
Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells
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[PMID: 18976908] |
| HepG2 | EC50 |
6.85 μM
Compound: NS-220
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Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells
Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells
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[PMID: 18976908] |
| HepG2 | EC50 |
7 μM
Compound: NS-220
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Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
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[PMID: 18805005] |
| HepG2 | EC50 |
7 μM
Compound: NS-220
|
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
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[PMID: 18805005] |
Chemical Information
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CAS No. 377731-45-8
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Masse moléculaire 373.44
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Formule C21H27NO5
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SMILES
O=C([C@]1(C)OC[C@H](CCCCC2=C(C)OC(C3=CC=C(C)C=C3)=N2)CO1)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Kenji Kuwabara, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose levels and modifies lipoprotein profiles in KK-Ay mice. J Pharmacol Exp Ther. 2004 Jun;309(3):970-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NS-220 Related Classifications
HY-19425 Related Classifications
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