Molecular structure of GSK 3787, CAS Number: 188591-46-0
GSK 3787 (CAS 188591-46-0)
See product citations (3)
Alternate Names:
4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide
Application:
GSK 3787 is a potent and selective peroxisome proliferatior-activated recepter δ antagonist
CAS Number:
188591-46-0
Purity:
≥99%
Molecular Weight:
392.78
Molecular Formula:
C15H12ClF3N2O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GSK 3787 is a selective PPARβ (peroxisome proliferator-activated receptor β) antagonist which binds to Cys249 in the PPARβ binding pocket. PPARβ is essential in the catabolism of fatty acids. Studies indicate that GSK 3787 antagonizes the agonistic effects of GW 0742 (sc-203991). This inhibits upregulation of Angptl4 and Adrp mRNA expression in mice colon. In addition, GSK 3787 acts in a dual role as a weak agonist and antagonist towards PPARγ. These studies suggest that GSK 3787 also functions as an antagonist towards PPARβ which has similar functions to PPARδ.
GSK 3787 (CAS 188591-46-0) References
- Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. | Shearer, BG., et al. 2010. J Med Chem. 53: 1857-61. PMID: 20128594
- Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787. | Palkar, PS., et al. 2010. Mol Pharmacol. 78: 419-30. PMID: 20516370
- JAZF1 regulates visfatin expression in adipocytes via PPARα and PPARβ/δ signaling. | Ming, GF., et al. 2014. Metabolism. 63: 1012-21. PMID: 24930994
- PPARδ signaling mediates the cytotoxicity of DHA in H9c2 cells. | Samokhvalov, V., et al. 2015. Toxicol Lett. 232: 10-20. PMID: 25300478
- IL-15 Mediates Mitochondrial Activity through a PPARδ-Dependent-PPARα-Independent Mechanism in Skeletal Muscle Cells. | Thornton, SM., et al. 2016. PPAR Res. 2016: 5465804. PMID: 27738421
- Peroxisome proliferator-activated receptor β/δ does not regulate glucose uptake and lactose synthesis in bovine mammary epithelial cells cultivated in vitro. | Lohakare, J., et al. 2018. J Dairy Res. 85: 295-302. PMID: 29941059
- PPARδ, a Potential Therapeutic Target for Heart Disease. | Yang, Q. and Long, Q. 2018. Nucl Receptor Res. 5: PMID: 31032335
- The interplay between non-esterified fatty acids and bovine peroxisome proliferator-activated receptors: results of an in vitro hybrid approach. | Busato, S. and Bionaz, M. 2020. J Anim Sci Biotechnol. 11: 91. PMID: 32793344
- Peroxisome Proliferator-Activated Receptor Activation in Precision-Cut Bovine Liver Slices Reveals Novel Putative PPAR Targets in Periparturient Dairy Cows. | Busato, S., et al. 2022. Front Vet Sci. 9: 931264. PMID: 35903133
- PPAR beta/delta regulates the immune response mechanisms in the porcine endometrium during LPS-induced inflammation - An in vitro study. | Golubska, M., et al. 2024. Theriogenology. 226: 130-140. PMID: 38878465
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D4DR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK 3787, 10 mg | sc-358241 | 10 mg | $145.00 | |||
GSK 3787, 50 mg | sc-358241A | 50 mg | $615.00 |