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T0901317

Catalog No. T6690   CAS 293754-55-9

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).

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T0901317 Chemical Structure
T0901317, CAS 293754-55-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 52.00
25 mg In stock $ 80.00
50 mg In stock $ 101.00
100 mg In stock $ 159.00
200 mg In stock $ 207.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 99.58%
Purity: 99.43%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).
Targets&IC50 LXR:50 nM(EC50), FXR:5 μM(EC50)
In vitro T0901317 acts through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. T0901317 upregulates expression of the ABCA1 gene associated with cholesterol efflux regulation and HDL metabolism.[1] T0901317 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. [2] T0901317, is also a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 induces expression not only of LXR target genes, but also of PXR target genes in cells and animals, including the scavenger receptor CD36. [3] T0901317 decreases amyloid-β production in primary neurons in vitro. [4] T0901317 is found to directly bind to RORα and RORγ with high affinity (Ki = 132 and 51 nM, respectively), resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 represses RORα/γ-dependent transactivation of ROR-responsive reporter genes and in HepG2 cells reduces recruitment of steroid receptor coactivator-2 by RORα at an endogenous ROR target gene (G6Pase). [5]
In vivo T0901317 treatment of 11-week-old APP23 mice for 6 days shows a significant increase in ABCA1 expression and a decrease in the ratio of soluble APP (sAPP)β- to sAPPα-cleavage products. Most importantly, the treatment causes a statistically significant reduction in the levels of soluble Aβ40 and of Aβ42 in the brain these mice. [4]
Molecular Weight 481.33
Formula C17H12F9NO3S
CAS No. 293754-55-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48.1 mg/mL (100 mM)

Ethanol: 48.1 mg/mL (100 mM)

TargetMolReferences and Literature

1. Repa JJ, et al. Science, 2000, 289(5484), 1524-1529. 2. Houck KA, et al. Mol Genet Metab, 2004, 83(1-2), 184-187. 3. Mitro N, et al. FEBS Lett, 2007, 581(9), 1721-1726. 4. Koldamova RP, et al. J Biol Chem, 2005, 280(6), 4079-4088. 5. Kumar N, et al. Mol Pharmacol, 2010, 77(2), 228-236. 6. Ding H et al. LXR agonist T0901317 upregulates thrombomodulin expression in glomerular endothelial cells by inhibition of nuclear factor κB. Mol Med Rep. 2016 Jun;13(6):4888-96 7. Liu N, Sun Q, Xu H, et al. Hyperuricemia induces lipid disturbances mediated by LPCAT3 upregulation in the liver[J]. The FASEB Journal. 2020, 34(10): 13474-13493.

TargetMolCitations

1. Li C, Wu H, Na H S T, et al. Neuronal-Microglial Liver X receptor β Activating Decrease Neuroinflammation and Chronic Stress-induced Depression-Related Behavior in Mice. Brain Research. 2022: 148112.

Related compound libraries

This product is contained In the following compound libraries:
Target-Focused Phenotypic Screening Library Lipid Metabolism Compound Library Nuclear Receptor Compound Library ReFRAME Related Library Orally Active Compound Library Bioactive Lipid Compound Library Anti-Neurodegenerative Disease Compound Library Apoptosis Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max

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Keywords

T0901317 293754-55-9 Apoptosis Metabolism Liver X Receptor FXR ROR orally fibroblasts LXRβ foreskin T 0901317 Liver X receptor atherosclerosis LDL SKOV3 inhibit NR1H4 carcinoma CaOV3 HS-68 RAR-related orphan receptor RORγ Inhibitor T-0901317 LXRα RORα A2780 LXR ovarian inhibitor

 

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