T0901317

SKU: orb1225409

Description

A potent, high affinity LXR agonist (EC50=50 nM, Kd 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 FXRs.Alzheimer's Disease Discontinued.

Key Properties

• CAS Number: 293754-55-9
• MW: 481.3327
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₂F₉NO₃S
• SMILES: OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(N(CC(F)(F)F)S(C2=CC=CC=C2)(=O)=O)C=C1
• Target: LXR
• Solubility: DMSO: ≥ 27 mg/mL

Bioactivity

• In Vivo:
  Animal model: 8-to 10-week-old LDL receptor null mice. Dosage: 10 mg/kg. Administration: Orally; daily; for 12 weeks. Result: Inhibited the progression of atherosclerosis.
• In Vitro:
  Cell Proliferation Assay Cell line: A2780, CaOV3 and SKOV3 ovarian cancer cell lines. Concentration: 5, 10, 20, 40 or 50 μM. Incubation time: 72 hours. Result: Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner. Cell Cycle Analysis Cell line: A2780, CaOV3 and SKOV3 cells. Concentration: 10 μM. Incubation time: 24, 48 or 72 hours. Result: Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase. Apoptosis Analysis Cell line: CaOV3 cells. Concentration: 10 to 40 μM. Incubation time: 24 hours. Result: Resulted in a significant increase of cells in early apoptosis. Western blot analysis. Cell line: CaOV3 cells. Concentration: 5 to 40 μM. Incubation time: 48 hours. Result: Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

T 0901317 | T-0901317

Quick Database Links

Gene Symbol

LXR