TO901317
From ToxBankWiki
Executive Summary Information
Compound | TO901317 (N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide) |
Toxicities | Steatosis |
Mechanisms | Dual liver X receptor (LXR) and pregnane X receptor (PXR) agonist. |
Comments | TO901317 is a standard for induction of steatosis via ligand-receptor mediated increases in of fatty acid synthesis, as opposed to inhibition of fatty acid oxidation by chemically reactive compounds. |
Feedback Contact | Gold Compound Working Group (GCWG) |
TO901317 | |
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Identifiers | |
Leadscope Id | LS-185184 |
CAS | 293754-55-9 |
Pathway DBs | |
Assay DBs | |
PubChem CID | 447912 |
Omics DBs | |
Properties | |
ToxCast Accepted | no |
Toxic Effect | Steatosis |
ToxBank Accepted | yes |
Approved on | 2011-06-28 |
- In Vivo Data
- PK-ADME Data
- 'Omics and IC50 Data
- Physical Properties
- Recommended Product and Source
- Additional Literature
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PubMed references
The following resource link will perform a PubMed query for the terms "TO901317" and "steatosis".
TO901317 Search
References
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The recommended source is Sigma Aldrich, product number T2320.
TO901317 | |
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Source | Sigma Aldrich |
Product ID | T2320 |
Mol Weight | 481.3 |
Purity | ≥98 % |
Quantity | 5 mg |
Cost | 72.30 USD |
Storage | −20°C |
- 1. Baranowski, Biological role of liver X receptors, Journal of Physiology and Pharmacology, 59 (Suppl 7), 31–55, 2008
- 2. Ory D.S., NR Signaling in the control of Cholesterol Homeostasis: Have the orphans found a home?, Circ. Res., 95, 660-670, 2004
- 3. Lund E.G., et al, Different roles of liver X receptor alpha and beta in lipid metabolism: effects of an alpha-selective and a dual agonist in mice deficient in each subtype, Biochem. Pharmacol., 71, 453–463, 2006
- 4. Chu K., et al, Stearoyl-coenzyme A desaturase 1 deficiency protects against hypertriglyceridemia and increase plasma high-density lipoprotein cholesterol induced by liver X receptor activation, Mol Cell Biol, 26. 6786-6798, 2006
- 5. Collins J.L., et al, Identification of a non-steroidal liver X receptor agonist through parallel array synthesis of tertiary amines, J Med Chem, 45, 1963-1966, 2002
- 6. Groot P.H., et al, Synthetic LXR agonists increase LDL in CETP species, J Lipid Res, 46, 2182-2191, 2005
- 7. Hu T., et al, Hepatic Peroxisomal Fatty Acid beta-Oxidation Is Regulated by Liver X Receptor alpha, Endocrinology, 146, 5380-5387, 2005
- 8. Jamroz-Wiśniewska A., et al, Liver X receptors (LXRs). Part II: non-lipid effects, role in pathology, and therapeutic implications, Postepy. Hig. Med. Dosw., 61, 760-85, 2007
- 9. Kase E.T., et al, Liver X receptor antagonist reduces lipid formation and increases glucose metabolism in myotubes from lean, obese and type 2 diabetic individuals. Diabetologia, 50, 2171-2180, 2007
- 10. Kotokorpi P., et al. Physiological differences between human and rat primary hepatocytes in response to liver X receptor activation by 3-[3-[N-(2-chloro-3-trifluoromethylbenzyl)-(2,2-diphenylethyl)amino]propyl oxy]phenylacetic acid hydrochloride (GW3965). Mol Pharmacol 72, 947-955, 2007
- 11. Laffitte B.A., et al, Activation of liver X receptor improves glucose tolerance through coordinate regulation of glucose metabolism in liver and adipose tissue. Proc. Natl. Acad. Sci. USA, 100, 5419–5424, 2003
- 12. Lazar M.A., Willson T.M., Sweet Dreams for LXR, Cell Metabolism, 5 (No 3), 159–161, 2007
- 13. LeBlanc G.A., et al, Draft Detailed Review Paper, State of the Science on Novel In Vitro and In Vivo Screening and Testing Methods and Endpoints for Evaluating Endocrine Disruptors, Contractor: RTI International, Draft #2, 2011
- 14. Lee J.H., et al, PRX and LXR in hepatic Steatosis: a new dog and an old dog with new tricks, Mol. Pharm., 5(No 1),60-66, 2008
- 15. Li Y., et al, Induction of human liver X receptor alpha gene expression via an autoregulatory loop mechanism. Mol. Endocrinol., 16, 506-514, 2002
- 16. Liang G., et al, Diminished hepatic response to fasting/refeeding and liver X receptor agonists in mice with selective deficiency of sterol regulatory element-binding protein-1c. J. Biol. Chem., 277, 9520–9528, 2002
- 17. Moya M., et al, Enhanced Steatosis by nuclear receptor ligands: A study in cultured human hepatocytes and hepatoma cells with a characterized nuclear receptor expression profile, Chemico-Biological Interactions, 184, 376-387, 2010
- 18. Oisterveer M. H., et al, The liver X receptor: Control of cellular lipid homeostasis and beyond Implications for drug design, Progress in Lipid Research, 49, 343–352, 2010
- 19. Olefsky J.M., Nuclear Receptor Minireview Series, J. Biol. Chem., 276 (No 40), 36863–36864, 2001
- 20. Pawar A., et al, The role of liver X receptor-alpha in the fatty acid regulation of hepatic gene expression. J. Biol. Chem. 278, 40736–40743.
- 21. Song C., Ubiquitous receptor: A receptor that modulates gene activation by retinoic acid and thyroid hormone receptors, Biochemistry, 91, 10809-10813, 1994
- 22. Williams S., et al, X-ray Crystal Structure of the Liver X Receptor Ligand Binding Domain, J. Biol. Chem., 278, 27138–27143, 2003