TH1020|1841460-82-9|-陌孚医药/Medlife

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TH1020

目录号: PL02319 纯度: ≥99%

CAS No. :1841460-82-9

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中文名称	TH1020
英文名称	TH1020
英文别名	4-((4-Benzyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)thio)pyrido[3′,2′,4,5]-thieno[3,2-d]pyrimidine;4-[[4-(Phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine;TH1020;TH 1020;4-[[4-(Phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3',2';4-((4-Benzyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)thio)pyrido[3',2':4,5]thieno[3,2-d]pyrimidine;4-((4-Benzyl-5-(pyridin4yl)-4H-1,2,4-triazol-3-yl)thio)pyrido[3',2':4,5]thieno[3,2-d]pyrimidine;TH1020, >=95% (HPLC);E75630;4-[[4-(Phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3',2':4,5]thieno[3,2-d]pyrimidine;6-[(4-be;CID 124203921;BDBM50552136;4-[[4-(Phenylmethyl)-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]thio]-pyrido[3',2':
Cas No.	1841460-82-9
分子式	C₂₃H₁₅N₇S₂
分子量	453.54
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TH1020 是一种有效的选择性的 Toll 样受体 5 (TLR5)/鞭毛蛋白复合拮抗剂，IC₅₀ 为 0.85 μM。TH1020 抑制鞭毛蛋白诱导的 TLR5 信号传导，对 TLR2，TLR3，TLR4，TLR7 和 TLR8 无效。
生物活性	TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC 50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.
性状	Solid
IC50 & Target[1][2]	IC50: 0.85 μM (toll-like receptor 5 (TLR5)/flagellin complex)
体外研究(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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
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.

溶解度数据	In Vitro: DMSO : 2 mg/mL (4.41 mM; ultrasonic and warming and adjust pH to 2 with 1M HCl and heat to 80°C)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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