T0901317

SKU: orb1300551

Description

T0901317 is a dual agonist of LXR and FXR with EC50 values of approximately 50 nM and 5 µM, respectively. It also acts as an inhibitor of NF-κB. This small molecule is a valuable research tool for studying nuclear receptor signaling and inflammation in metabolic and liver disease models, both in vitro and in vivo.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 293754-55-9
• MW: 481.33
• Purity: 99.64% (May vary between batches)
• Formula: C₁₇H₁₂F₉NO₃S
• SMILES: C(C(F)(F)F)(C(F)(F)F)(O)C1=CC=C(N(S(=O)(=O)C2=CC=CC=C2)CC(F)(F)F)C=C1
• Target: Liver X Receptor,Apoptosis,FXR,ROR
• Solubility: Ethanol:48.1 mg/mL (99.93 mM);DMSO:130 mg/mL (270.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (5.19 mM)

Bioactivity

• Target IC50:
  LXR:50 nM(EC50)|FXR:5 μM(EC50)
• 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.
• 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. 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. 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. T0901317 decreases amyloid-β production in primary neurons in vitro. 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

447912