1841460-82-9
中文名稱
TH1020
英文名稱
TH1020
CAS
1841460-82-9
分子式
C23H15N7S2
分子量
453.54
MOL 文件
1841460-82-9.mol
更新日期
2024/12/23 09:08:09
1841460-82-9 結(jié)構(gòu)式
基本信息
中文別名
化合物TH10204-((4-芐基-5-(吡啶-4-基)-4H-1,2,4-三唑-3-基)硫基)吡啶并[3',2':4,5]噻吩并[3,2-D]嘧啶
英文別名
TH1020TH1020 >=95% (HPLC)
4-[[4-(Phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3',2'
4-[[4-(Phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3',2':4,5]thieno[3,2-d]pyrimidine
物理化學(xué)性質(zhì)
沸點765.8±70.0 °C(Predicted)
密度1.51±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度Chloroform: 1 mg/ml
酸度系數(shù)(pKa)1.92±0.10(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
TH1020 是一種有效的選擇性的 Toll 樣受體 5 (TLR5)/鞭毛蛋白復(fù)合拮抗劑,IC50 為 0.85 μM。TH1020 抑制鞭毛蛋白誘導(dǎo)的 TLR5 信號傳導(dǎo),對 TLR2,TLR3,TLR4,TLR7 和 TLR8 無效。靶點
IC50: 0.85 μM (toll-like receptor 5 (TLR5)/flagellin complex)
體外研究
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.
The IL-17C secretion is almost completely abolished by TH1020 (0.5 μM) in bacterial strain C83901 infected IPEC-J2 cells.
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.