ITE - Aryl Hydrocarbon Receptor Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEITECat. No.: HY-19317CAS No.: 448906-42-1分式: CHNOS分量: 286.31作靶點(diǎn): Aryl Hydrocarbon Receptor作通路: Immunology/Inflammation儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 41 mg/mL (143.20 mM)H2O

2、 : 90% corn oilSolubility: 2.67 mg/mL (9.33 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 ITE種有效的內(nèi) 性芳烴受體 (AhR) 激動(dòng)劑，能夠直接與 AHR 結(jié)合，Ki 值為 3 nM。ITE 具有免疫抑制作。IC50 & Target Ki: 3 nM (AhR) 1體外研究 ITE is an endogenous agonist of AhR, binding directly to AHR, with a

3、Ki of 3 nM 1. ITE (0.03-30 mg/mL)decreases the antigen-specific T-cell proliferative responses 2. ITE potently inhibits human pulmonaryartery endothelial (HPAECs) growth at 10 and 20 M, but shows no effect at 0.01-5 M. ITE does not affectcell cycle progress of HPAECs at 10 and 20 M, or induce expres

4、sion of cleaved caspase-3 protein inHPAECs at 20 M. In addition, ITE (20 M) elevates CYP1A1 and CYP1B1 mRNA levels and decreases thelevels of AhR protein in HPAECs 3.體內(nèi)研究 ITE (200 g, i.p.) significantly suppresses the development of experimental autoimmune uveitis (EAU) inmice. ITE reduces the propo

5、rtions of cells expressing IFN-, IL-17, or IL-10 in mice. ITE also suppresses thesecretion of inflammatory cytokines by LN cells in mice 2.PROTOCOLCell Assay 3 Subconfluent cells (25, 000 cells/well) are seeded in 96-well plates. Cells are treated with ITE at 5, 10 and 20M or DMSO (0.1% v/v) in ECM

6、for 2, 4 or 6 days with a change of ECM containing DMSO or ITE everyother day (5 wells/treatment). At the end of treatment, cells are incubated with MTT reagent for 4 hr, andsolubilized in crystal dissolving solution (100 L/well) for 20 min. The absorbance is determined at 570 nmusing the microplate

7、 reader 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 Eight- to 12-week-old female B10.A mice is used in the assay. Daily treatment starts on day 0 and consists of200 g of ITE suspended in 0.2 mL PBS, given intraperiton

8、eally. Control mice are similarly treated with 0.2mL of the vehicle, PBS containing 3.6% DMSO 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Song J, et al. A ligand for the aryl hydrocarbon receptor isolated from lung. Proc Natl Acad Sci

9、 U S A. 2002 Nov 12;99(23):14694-9.2. Nugent LF, et al. ITE, a novel endogenous nontoxic aryl hydrocarbon receptor ligand, efficiently suppresses EAU and T-cell-mediatedimmunity. Invest Ophthalmol Vis Sci. 2013 Nov 13;54(12):7463-9.3. Pang LP, et al. ITE inhibits growth of human pulmonary artery endothelial cells. Exp Lung Res. 2017 Oct;43(8):283-292.McePdfHeightCaution: Product has not been fully validated for me