TH1020|CAS 1841460-82-9|DC Chemicals

Cas No.:	1841460-82-9
Chemical Name:	4-((4-Benzyl-5-(pyridin4yl)-4H-1,2,4-triazol-3-yl)thio)pyrido[3',2':4,5]thieno[3,2-d]pyrimidine
Synonyms:	TH1020; TH-1020; TH 1020.
SMILES:	C12=NC=NC(SC3=NN=C(N3CC4=CC=CC=C4)C5=CC=NC=C5)=C1SC6=NC=CC=C62
Formula:	C₂₃H₁₅N₇S₂
M.Wt:	453.54
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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. [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.

Description:	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].
Target:	IC50: 0.85 μM (toll-like receptor 5 (TLR5)/flagellin complex)[1]
In Vitro:	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].
References:	[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. [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.

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