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 No.: 196809-22-0
- Formule: C29H28N2O6
- Masse moléculaire:500.54
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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
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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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.
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[PMID: 11720854] |
| CV-1 | EC50 |
3500 nM
Compound: GW-7845
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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.
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[PMID: 11720854] |
Chemical Information
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CAS No. 196809-22-0
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Masse moléculaire 500.54
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Formule 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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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]. 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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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