L-Kynurenine - Aryl Hydrocarbon Receptor Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEL-KynurenineCat. No.: HY-104026CAS No.: 2922-83-0分式: CHNO分量: 208.21作靶点: Aryl Hydrocarbon Receptor; Endogenous Metabolite作通路: Immunology/Inflammation; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 m

2、onths-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (240.14 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.8028 mL 24.0142 mL 48.0284 mL5 mM 0.9606 mL 4.8028 mL 9.6057 mL10 mM 0.4803 mL 2.4014 mL 4.8028 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制

3、澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (12.01 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (12.01 mM); Clear solution3. 请依

4、序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (12.01 mM); Clear solution; Need warming1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 L-KynurenineL-氨酸的代谢物。它 种芳烃受体 (aryl hydrocarbon receptor) 激动剂。IC50 & Target Human Endogenous Metabolite体外研究 Kynurenine and its further br

5、eakdown products carry out diverse biological functions, including dilating bloodvessels during inflammation and regulating the immune response. Some cancers increase kynurenineproduction, which increases tumor growth. L-kynurenine (Kyn) is an aryl hydrocarbon receptor (AHR) agonistthat activates AH

6、R-directed, naive T cell polarization to the anti-inflammatory Treg phenotype. Kynurenineactivates AHR signaling at physiological concentrations in H1L7.5c3 cells and acts as an AHR agonist after a24-hr exposure by inducing the AHR-regulated luciferase gene in H1L7.5c3 mouse hepatocyte cells 1.体内研究

7、Kynurenine dilates arteries from rats as well as humans via Kv7 channels in the vascular smooth muscle. Inrats, this tryptophan metabolite causes hypotension, which is partly counteracted by Kv7 channel inhibition2. L-kynurenine administered 1 h before the hypoxia-ischemia shows a dose-dependent sig

8、nificantneuroprotective effect, with complete protection at a dose of 300 mg/kg. The induction of c-fosimmunoreactivity in cerebral cortex is also blocked by this dose of L-kynurenine 3.PROTOCOLCell Assay 1 Luciferase assays are carried out using the H1L7.5c3 cells. At the indicated times (0.5, 2, 4

9、, 6, 12, 18, 24 h)and concentrations (0.1, 1, 10, 100 M) of exposures to Kynurenine, cells are removed from incubation andallowed to equilibrate to room temperature for 15min. After equilibration, the medium is removed and thecells are washed twice with at room temperature with DPBS. The cells are l

10、ysed with 20 L/well 1 PassiveLysis Buffer and shaken for 20min at room temperature. Luciferase activity is recorded using anLuminometer Microplate Reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 3Administration 3 The effects of incr

11、easing doses of L-kynurenine with or without probenecid on concentrations of kynurenicacid in cerebral cortex are examined in 7-day-old rats. Six animals are examined in each group. Animals aretreated with L-kynurenine at doses of 100, 200, 300, and 400 mg/kg or kynurenine, 200 mg/kg withprobenecid,

12、 50 mg/kg. Animals are killed at 1 h, the brains promptly removed, and the cerebral cortex isdissected and placed in 0.5 mL of chilled 0. 1 M HCl. Kynurenic acid measurements are made by high-performance liquid chromatography with fluorescence detection. Protein measurements are made using afluorome

13、tric assay 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Moyer BJ, et al. Inhibition of the aryl hydrocarbon receptor prevents Western diet-induced obesity. Model for AHR activation by2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEkyn

14、urenine via oxidized-LDL, TLR2/4, TGF, and IDO1. Toxicol Appl Pharmacol. 2016 Jun 1;300:13-24.2. Sakakibara K, et al. Kynurenine causes vasodilation and hypotension induced by activation of KCNQ-encoded voltage-dependent K(+)channels. J Pharmacol Sci. 2015 Sep;129(1):31-7.3. Nozaki K, et al. Neuroprotective effects of L-kynurenine on hypoxia-ischemia and NMDA lesions in neonatal rats. J Cereb Blood FlowMetab. 1992 M