AT791

SKU: orb1688156

Description

AT791 is an orally bioavailable small molecule inhibitor of Toll-like receptors 7 and 9 (TLR7/9). It is used in research to investigate autoimmune pathways, particularly in lupus models, by suppressing TLR-mediated signaling in both cellular assays and in vivo studies.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 1219962-49-8
• MW: 397.51
• Purity: 99.88% (May vary between batches)
• Formula: C₂₃H₃₁N₃O₃
• SMILES: N1=C(OC=2C=C(OCCCN(C)C)C=CC12)C3=CC=C(OCCCN(C)C)C=C3
• Target: TLR
• Solubility: DMSO:80 mg/mL (201.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.3 mM)

Bioactivity

• Target IC50:
  TLR7:3.33μM|TLR9:0.04μM
• In Vivo:
  Short-term induction of serum interleukin-6 by CpG1668 DNA in mice could be effectively inhibited by pretreatment with AT791 (20 mg/kg).
• In Vitro:
  AT791 effectively inhibited DNA stimulation of HEK:TLR9 cells with an IC50 value of 40 nM, respectively, but was significantly less effective in inhibiting LPS endotoxin stimulation of HEK:TLR4 cells or R848 HEK:TLR7 cells. Methods: To confirm whether the interaction of AT791 with DNA was associated with its ability to inhibit DNA-TLR9 interaction in cells, a live cell version of the oligonucleotide bait assay was developed. A non-stimulatory version of the oligonucleotide CpG2216 was created by inverting the stimulatory CpG motif to GpC to generate GpC2216. Results: Stimulatory CpG2216 induced IL-6 production in BMDCs, whereas AT791 (10 mM) inhibited this production. However, when an excess of non-stimulatory GpC2216 was added, IL-6 induction was restored. GpC2216 itself, either alone or in the presence of AT791, does not stimulate IL-6 production.
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Storage & Handling

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

Alternative Names

AT 791

Compound Identifiers

PubChem CID

45256283