中文名称:

ITE

中文同义词:

2-(1H-吲哚-3-基羰基)-4-噻唑羧酸甲酯;芳香烃受体(AHR)激动剂(ITE)

英文名称:

ITE

英文同义词:

ITE;2-(1H-INDOL-3-YLCARBONYL)-4-THIAZOLECARBOXYLIC ACID METHYL ESTER;2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXYLIC ACID;2-(1H-indole-37-carbonyl)-thiasole-4-carboxylic acid methyl ester;Methyl 2-(1H-indole-3-carbonyl)thiazole-4-carboxylate;methyl 2-(1H-indole-3-carbonyl)-1,3-thiazole-4-carboxylate;ARYL HYDROCARBON RECEPTOR LIGAND;4-Thiazolecarboxylic acid, 2-(1H-indol-3-ylcarbonyl)-, methyl ester

CAS号:

448906-42-1

分子式:

C14H10N2O3S

分子量:

286.31

EINECS号:

相关类别:

细胞生物学试剂;化工原料

Mol文件:

448906-42-1.mol

沸点 

520.4±48.0 °C(Predicted)

密度 

1.427±0.06 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: 30 mg/mL, soluble

形态

solid

酸度系数(pKa)

14.38±0.30(Predicted)

简介

ITE是一种芳香烃受体(AhR)激动剂,Ki值为3nM,ITE作用于OVCAR-3细胞增殖为,IC50值为0.2nM。

生物活性

ITE 是一种有效的内源性芳香烃受体 (AhR) 激动剂，能够直接与 AHR 结合，Ki 值为 3 nM。ITE 具有免疫抑制作用。

靶点

Ki: 3 nM (AhR)

体外研究

ITE is an endogenous agonist of AhR, binding directly to AHR, with a K i of 3 nM. ITE (0.03-30 mg/mL) decreases the antigen-specific T-cell proliferative responses. ITE potently inhibits human pulmonary artery endothelial (HPAECs) growth at 10 and 20 µM, but shows no effect at 0.01-5 µM. ITE does not affect cell cycle progress of HPAECs at 10 and 20 µM, or induce expression of cleaved caspase-3 protein in HPAECs at 20 µM. In addition, ITE (20 µM) elevates CYP1A1 and CYP1B1 mRNA levels and decreases the levels of AhR protein in HPAECs.

体内研究

ITE (200 μg, i.p.) significantly suppresses the development of experimental autoimmune uveitis (EAU) in mice. ITE reduces the proportions of cells expressing IFN-γ, IL-17, or IL-10 in mice. ITE also suppresses the secretion of inflammatory cytokines by LN cells in mice.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26-36

WGK Germany 

3