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TH1020

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Chemical Structure| 1841460-82-9 同义名 : -
CAS号 : 1841460-82-9
货号 : A1340564
分子式 : C23H15N7S2
纯度 : 99%+
分子量 : 453.542
MDL号 : MFCD30480930
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 2 mg/mL(4.41 mM),配合低频超声,水浴加热至45℃,并调节pH至2,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 TH1020 is a potent and selective TLR5/flagellin complex antagonist with an IC50 value of 0.85 μM. TH1020 inhibits flagellin-induced TLR5 signalling, and is inactive against TLR2, TLR3, TLR4, TLR7, and TLR8[1].TH1020 disrupts the binding of flagellin to TLR5 and inhibits downstream signalling mediated by the formation of the TLR5/flagellin complex. At 0.37 μM, TH1020 almost completely inhibited TLR5-mediated TNF-α secretion[1].In bacterial strain C83901-infected IPEC-J2 cells, TH1020 almost completely inhibited IL-17C secretion at a concentration of 0.5 μM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL

参考文献

[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.