Molecular structure of XCT790, CAS Number: 725247-18-7
XCT790 (CAS 725247-18-7)
Alternate Names:
3-[4-(2,4-bis-trifluoromethylbenzyloxy)-3-methoxyphenyl]-2-cyano-n-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)acrylamide
Application:
XCT790 is a potent inverse agonist of ERRα
CAS Number:
725247-18-7
Purity:
≥98%
Molecular Weight:
596.42
Molecular Formula:
C23H13F9N4O3S
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
This is a potent and specific inverse agonist of ERRα. XCT790 is a selective, which shows no significant antagonist activity on related nuclear receptors, such as ERR or ERα at concentrations below 10 µM. This also inhibits the constitutive activity of ERRα in both biochemical and cell-based assays. The IC50 value is 300-500 nM in transient transfection assays using GAL4-ERR LBD or full-length ERR with the mSHP promoter.
XCT790 (CAS 725247-18-7) References
- Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. | Busch, BB., et al. 2004. J Med Chem. 47: 5593-6. PMID: 15509154
- Identification and characterization of estrogen receptor-related receptor alpha and gamma in human glioma and astrocytoma cells. | Gandhari, MK., et al. 2010. Mol Cell Endocrinol. 315: 314-8. PMID: 19822186
- Estrogen-related receptor alpha and PGC-1-related coactivator constitute a novel complex mediating the biogenesis of functional mitochondria. | Mirebeau-Prunier, D., et al. 2010. FEBS J. 277: 713-25. PMID: 20067526
- A Role for the orphan nuclear receptor estrogen-related receptor alpha in endometrial stromal cell decidualization and expression of genes implicated in energy metabolism. | Bombail, V., et al. 2010. J Clin Endocrinol Metab. 95: E224-8. PMID: 20668045
- Estrogen-related receptor α regulates skeletal myocyte differentiation via modulation of the ERK MAP kinase pathway. | Murray, J. and Huss, JM. 2011. Am J Physiol Cell Physiol. 301: C630-45. PMID: 21562305
- The corepressor NCoR1 antagonizes PGC-1α and estrogen-related receptor α in the regulation of skeletal muscle function and oxidative metabolism. | Pérez-Schindler, J., et al. 2012. Mol Cell Biol. 32: 4913-24. PMID: 23028049
- Estrogen-related receptor alpha modulates lactate dehydrogenase activity in thyroid tumors. | Mirebeau-Prunier, D., et al. 2013. PLoS One. 8: e58683. PMID: 23516535
- The estrogen-related receptor α inverse agonist XCT 790 is a nanomolar mitochondrial uncoupler. | Eskiocak, B., et al. 2014. Biochemistry. 53: 4839-46. PMID: 24999922
- Novel endocrine therapeutic strategy in endometrial carcinoma targeting estrogen-related receptor α by XCT790 and siRNA. | Sun, P., et al. 2018. Cancer Manag Res. 10: 2521-2535. PMID: 30127640
- ERRα promotes breast cancer cell dissemination to bone by increasing RANK expression in primary breast tumors. | Vargas, G., et al. 2019. Oncogene. 38: 950-964. PMID: 30478447
- Regulation of PGC-1α expression by a GSK-3β-TFEB signaling axis in skeletal muscle. | Theeuwes, WF., et al. 2020. Biochim Biophys Acta Mol Cell Res. 1867: 118610. PMID: 31738957
- Gremlin-1 augments the oestrogen-related receptor α signalling through EGFR activation: implications for the progression of breast cancer. | Park, SA., et al. 2020. Br J Cancer. 123: 988-999. PMID: 32572171
- Exploring the binding mode and thermodynamics of inverse agonists against estrogen-related receptor alpha. | Karnati, KR., et al. 2020. RSC Adv. 10: 16659-16668. PMID: 35498853
Substrate of:
ERR alpha.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
XCT790, 5 mg | sc-253835 | 5 mg | $176.00 |