GW7845
GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC50 of 3 μM by using Ba2+ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrial membrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells.
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- CAS 番号: 196809-22-0
- 分子式: C29H28N2O6
- 分子量:500.54
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Calcium Channel アイソフォーム固有の製品をすべて表示
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生物活性
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PPARγ |
L-type calcium channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
0.71 nM
Compound: GW-7845
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Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
|
[PMID: 11720854] |
| CV-1 | EC50 |
3500 nM
Compound: GW-7845
|
Maximal reporter activity against human Peroxisome proliferator activated receptor alpha Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
Maximal reporter activity against human Peroxisome proliferator activated receptor alpha Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
|
[PMID: 11720854] |
化学情報
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CAS 番号 196809-22-0
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分子量 500.54
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分子式 C29H28N2O6
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SMILES
O=C([C@H](CC1=CC=C(C=C1)OCCC2=C(OC(C3=CC=CC=C3)=N2)C)NC4=CC=CC=C4C(OC)=O)O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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]. Thomas J Heppner, et al. Novel PPARgamma agonists GI 262570, GW 7845, GW 1929, and pioglitazone decrease calcium channel function and myogenic tone in rat mesenteric arteries. Pharmacology. 2005 Jan;73(1):15-22. [Content Brief]
[2]. Jennifer J Schlezinger, et al. An L-tyrosine derivative and PPARgamma agonist, GW7845, activates a multifaceted caspase cascade in bone marrow B cells. Toxicol Sci. 2007 Jul;98(1):125-36. [Content Brief]
[3]. N Suh, et al. A new ligand for the peroxisome proliferator-activated receptor-gamma (PPAR-gamma), GW7845, inhibits rat mammary carcinogenesis. Cancer Res. 1999 Nov 15;59(22):5671-3. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)