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Submit ReviewXCT 790 is a selective ERRα inverse agonist (IC50 = ~400 nM). Displays no antagonist activity at ERRγ or ERα at concentrations below 10 μM. Interferes with PPARγ coactivator-1α (PGC-1α)/ERRα-dependent signaling: inhibits PGC-1α induction of ERRα and MAO-B gene expression and downregulates the constitutive transcriptional activity of ERRα in numerous cell lines.
分子量 | 596.42 |
公式 | C23H13F9N4O3S |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 725247-18-7 |
PubChem ID | 6918788 |
InChI Key | HQFNFOOGGLSBBT-AWNIVKPZSA-N |
Smiles | O=C(NC3=NN=C(C(F)(F)F)S3)/C(C#N)=C/C(C=C2OC)=CC=C2OCC1=C(C(F)(F)F)C=C(C(F)(F)F)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 5.96 | 10 温和加热 |
以下数据基于产品分子量 596.42。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 16.77 mL | 83.83 mL | 167.67 mL |
0.5 mM | 3.35 mL | 16.77 mL | 33.53 mL |
1 mM | 1.68 mL | 8.38 mL | 16.77 mL |
5 mM | 0.34 mL | 1.68 mL | 3.35 mL |
参考文献是支持产品生物活性的出版物。
Lanvin et al (2007) Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-alpha degradation by the estrogen receptor-related receptor-α inverse agonist XCT790. J.Biol.Chem. 282 28328 PMID: 17631492
Kong et al (2009) Peroxisome proliferator-activated receptor γ coactivator-1α enhances antiproliferative activity of 5'-deoxy-5-fluorouridine in cancer cells through induction of uridine phosphorylase. Mol.Pharmacol. 76 854 PMID: 19602572
Willy et al (2004) Regulation of PPARγ coactivator 1α (PGC-1α) signaling by an estrogen-related receptor alpha (ERRα) ligand. Proc.Natl.Acad.Sci.USA 101 8912
Theodoris et al (2021) Network-based screen in iPSC-derived cells reveals therapeutic candidate for heart valve disease. Science. 371 PMID: 33303684
If you know of a relevant reference for XCT 790, please let us know.
关键词: XCT 790, XCT 790 supplier, XCT790, ERRalpha, ERRa, ERRα, antagonists, inverse, agonists, PPARγ, PPARg, PPARgamma, coactivator-1α, coactivator-1alpha, coactivator-1a, PGC-1α, PGC-1alpha, PGC-1a, signaling, signalling, Estrogen, and, Related, Receptors, 3928, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 XCT 790 的部分引用包括:
Teng et al (2014) Development of a stable cell line with an intact PGC-1α/ERRα axis for screening environmental chemicals. Mol Cancer 444 177 PMID: 24457025
Núria et al (2021) The Nuclear Receptor ESRRA Protects from Kidney Disease by Coupling Metabolism and Differentiation. Cell Metab 33 379-394.e8 PMID: 33301705
Michael P et al (2015) Estrogen related receptor α (ERRα) a promising target for the therapy of adrenocortical carcinoma (ACC). Oncotarget 6 25135-48 PMID: 26312764
Hwang et al (2014) Estrogen-related receptor α is required for efficient human cytomegalovirus replication. Proc Natl Acad Sci U S A 111 E5706 PMID: 25512541
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