TH1020 

TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC₅₀ of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8^[1].

TH1020 inhibits the downstream signaling transduction mediated by the formation of the TLR5/Flagellin complex. TH1020 is suggested to compete with flagellin and disrupt its association with TLR5. TH1020 almost completely abolishes the TLR5-mediated TNF-α secretion at 0.37 μM^[1].
The IL-17C secretion is almost completely abolished by TH1020 (0.5 μM) in bacterial strain C83901 infected IPEC-J2 cells^[2].
Blocking TLR5 with TH1020 (0.5 μM) dramatically inhibits porcine beta-defensin (pBD)-2, claudin-1 and -2 mRNA expression in C83091 infected IPEC-J2 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

453.54

C₂₃H₁₅N₇S₂

1841460-82-9

Solid

Light yellow to yellow

C12=NC=NC(SC3=NN=C(N3CC4=CC=CC=C4)C5=CC=NC=C5)=C1SC6=NC=CC=C62

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Lei Yan, et al. Pyrimidine Triazole Thioether Derivatives as Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitors. ChemMedChem. 2016 Apr 19;11(8):822-6.  [Content Brief]

  [2]. Yu Luo, et al. Toll-like Receptor 5-mediated IL-17C Expression in Intestinal Epithelial Cells Enhances Epithelial Host Defense Against F4 + ETEC Infection. Vet Res. 2019 Jun 20;50(1):48.  [Content Brief]