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Submit ReviewT 0901317 is a potent, high affinity liver X receptor (LXR) agonist (EC50 ~ 50 nM, Kd values are 7 and 22 nM for LXR-α and LXR-β respectively). Upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism. Decreases amyloid-β production in primary neurons in vitro. Displays an EC50 of ~ 5 μM for activation of bile acid farnesoid X receptors (FXRs); 10-fold more potent than natural FXR ligand chenodeoxycholic acid. Also exhibits inverse agonist activity at constitutive androstane receptors (CAR).
T 0901317 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 481.33 |
公式 | C17H12F9NO3S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 293754-55-9 |
PubChem ID | 447912 |
InChI Key | SGIWFELWJPNFDH-UHFFFAOYSA-N |
Smiles | OC(C1=CC=C(C=C1)N(CC(F)(F)F)S(=O)(=O)C1=CC=CC=C1)(C(F)(F)F)C(F)(F)F |
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 | 48.13 | 100 | |
ethanol | 48.13 | 100 |
以下数据基于产品分子量 481.33。 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 |
---|---|---|---|
1 mM | 2.08 mL | 10.39 mL | 20.78 mL |
5 mM | 0.42 mL | 2.08 mL | 4.16 mL |
10 mM | 0.21 mL | 1.04 mL | 2.08 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Repa et al (2000) Regulation of absorption and ABC1-mediated efflux of cholesterol by RXR heterodimers. Science 289 1524 PMID: 10968783
Koldamova et al (2005) The liver X receptor ligand T0901317 decreases amyloid β production in vitro and in a mouse model of Alzheimer's disease. J.Biol.Chem. 280 4079 PMID: 15557325
Houck et al (2004) T0901317 is a dual LXR/FXR agonist. Mol.Gen.Metab. 83 184
Mitro et al (2007) The nuclear receptor LXR is a glucose sensor. Nature Lett. 445 219
Kanno et al (2013) T0901317, a potent LXR agonist, is an inverse agonist of CAR. J.Toxicol.Sci. 38 309 PMID: 23665929
If you know of a relevant reference for T 0901317, please let us know.
关键词: T 0901317, T 0901317 supplier, Potent, liver, X, receptor, LXR, agonists, FXR, Receptors, Liver, Farnesoid, LXR-like, T0901317, Constitutive, Androstane, Receptor, 2373, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 T 0901317 的部分引用包括:
Kasmi (2018) Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis. Nat Commun 9 1393 PMID: 29643332
Kim et al (2016) The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation Scientific Reports 6 37280 PMID: 27869139
Singh et al (2016) The fatty acid synthase inhibitor platensimycin improves Ins resistance without inducing liver steatosisin mice and monkeys PLoS One 11 e0164133 PMID: 27695056
Wahlang et al (2014) Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture. Toxicol Sci 140 283 PMID: 24812009
Candelaria et al (2014) Antiproliferative effects and mechanisms of liver X receptor ligands in pancreatic ductal adenocarcinoma cells. J Biomol Screen 9 e106289 PMID: 25184494
Herold (2017) Liver X receptor activation promotes differentiation of regulatory T cells. PLoS One 12 e0184985 PMID: 28926619
Bonney (2017) Differential Effects of Retinoic Acid Concentrations in Regulating Blood-Brain Barrier Properties. Eneuro 4 PMID: 28560318
Paterniti (2017) Liver X receptors activation, through TO901317 binding, reduces neuroinflammation in Parkinson's disease. PLoS One 12 e0174470 PMID: 28369131
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