中文名 | ITE |
英文名 | methyl 2-(1H-indole-3-carbonyl)thiazole-4-carboxylate |
别名 | 化合物ITE 芳香烃受体(AHR)激动剂(ITE) 2-(1H-吲哚-3-基羰基)-4-噻唑羧酸甲酯 |
英文别名 | ITE ARYL HYDROCARBON RECEPTOR LIGAND methyl 2-(1H-indole-3-carbonyl)thiazole-4-carboxylate Methyl 2-(1H-indole-3-carbonyl)thiazole-4-carboxylate 2-(1'H-INDOLE-3'-CARBONYL)-THIAZOLE-4-CARBOXYLIC ACID methyl 2-(1H-indole-3-carbonyl)-1,3-thiazole-4-carboxylate 2-(1H-INDOL-3-YLCARBONYL)-4-THIAZOLECARBOXYLIC ACID METHYL ESTER 2-(1'H-indole-37-carbonyl)-thiasole-4-carboxylic acid methyl ester 4-Thiazolecarboxylic acid, 2-(1H-indol-3-ylcarbonyl)-, methyl ester |
CAS | 448906-42-1 |
化学式 | C14H10N2O3S |
分子量 | 286.31 |
密度 | 1.427±0.06 g/cm3(Predicted) |
熔点 | 234 - 236°C |
沸点 | 520.4±48.0 °C(Predicted) |
溶解度 | DMSO: 30mg/ml,可溶 |
酸度系数 | 14.38±0.30(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | Off-White to Light Yellow |
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 - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
WGK Germany | 3 |
参考资料 展开查看 | 1: Henry, E.C., Bemis, J.C., Henry, O., et al. A potential endogenous ligand for the aryl hydrocarbon receptor has potent agonist activity in vitro and in vivo. Arch. Biochem. Biophys. 450(1), 67-77 (2006). 2: Yoshida, T., Katsuya, K., Oka, T., et al. Effects of AhR ligands on the production of immunoglobulins in purified mouse B cells. Biomed. Res. 33(2), 67-74 (2012). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.493 ml | 17.464 ml | 34.927 ml |
5 mM | 0.699 ml | 3.493 ml | 6.985 ml |
10 mM | 0.349 ml | 1.746 ml | 3.493 ml |
5 mM | 0.07 ml | 0.349 ml | 0.699 ml |
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