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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 377731-45-8
- 分子式: C21H27NO5
- 分子量:373.44
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
PPARα 19 nM (EC50) |
PPARγ 9.6 μM (EC50) |
PPARδ >1 mM (EC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
>100 μM
Compound: 14d, NS-220
|
Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay
|
[PMID: 17964792] |
| CV-1 | EC50 |
0.01 μM
Compound: 14d, NS-220
|
Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay
|
[PMID: 17964792] |
| CV-1 | EC50 |
0.03 μM
Compound: 14d, NS-220
|
Agonist activity at mouse PPARalpha expressed in CV1 cells by transactivation assay
Agonist activity at mouse PPARalpha expressed in CV1 cells by transactivation assay
|
[PMID: 17964792] |
| CV-1 | EC50 |
9.6 μM
Compound: 14d, NS-220
|
Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay
|
[PMID: 17964792] |
| HepG2 | EC50 |
0.052 μM
Compound: NS-220
|
Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells
Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells
|
[PMID: 18976908] |
| HepG2 | EC50 |
6.85 μM
Compound: NS-220
|
Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells
Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells
|
[PMID: 18976908] |
| HepG2 | EC50 |
7 μM
Compound: NS-220
|
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
|
[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
|
[PMID: 18805005] |
化学情報
-
CAS 番号 377731-45-8
-
分子量 373.44
-
分子式 C21H27NO5
-
SMILES
O=C([C@]1(C)OC[C@H](CCCCC2=C(C)OC(C3=CC=C(C)C=C3)=N2)CO1)O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)