L-Kynurenine-d4-1 is deuterium labeled L-Kynurenine. L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
212.24
Formula
C10H8D4N2O3
CAS 号
194546-33-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Moyer BJ, et al. Inhibition of the aryl hydrocarbon receptor prevents Western diet-induced obesity. Model for AHR activation by kynurenine via oxidized-LDL, TLR2/4, TGFβ, and IDO1. Toxicol Appl Pharmacol. 2016 Jun 1;300:13-24.
[3]. 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.
[4]. Nozaki K, et al. Neuroprotective effects of L-kynurenine on hypoxia-ischemia and NMDA lesions in neonatal rats. J Cereb Blood Flow Metab. 1992 May;12(3):400-7.
L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
IC50 & Target
Human Endogenous Metabolite
体外研究 (In Vitro)
Kynurenine and its further breakdown products carry out diverse biological functions, including dilating blood vessels during inflammation and regulating the immune response. Some cancers increase kynurenine production, which increases tumor growth. L-kynurenine (Kyn) is an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype. Kynurenine activates AHR signaling at physiological concentrations in H1L7.5c3 cells and acts as an AHR agonist after a 24-hr exposure by inducing the AHR-regulated luciferase gene in H1L7.5c3 mouse hepatocyte cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Kynurenine dilates arteries from rats as well as humans via Kv7 channels in the vascular smooth muscle. In rats, this tryptophan metabolite causes hypotension, which is partly counteracted by Kv7 channel inhibition[2]. L-kynurenine administered 1 h before the hypoxia-ischemia shows a dose-dependent significant neuroprotective effect, with complete protection at a dose of 300 mg/kg. The induction of c-fos immunoreactivity in cerebral cortex is also blocked by this dose of L-kynurenine[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
208.21
Formula
C10H12N2O3
CAS 号
2922-83-0
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
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
H2O : 20 mg/mL (96.06 mM; Need ultrasonic)
DMSO : 12.5 mg/mL (60.04 mM; ultrasonic and warming and heat to 60°C)
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Moyer BJ, et al. Inhibition of the aryl hydrocarbon receptor prevents Western diet-induced obesity. Model for AHR activation by kynurenine via oxidized-LDL, TLR2/4, TGFβ, 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 Flow Metab. 1992 May;12(3):400-7.
Cell Assay [1]
Luciferase assays are carried out using the H1L7.5c3 cells. At the indicated times (0.5, 2, 4, 6, 12, 18, 24 h) and concentrations (0.1, 1, 10, 100 μM) of exposures to Kynurenine, cells are removed from incubation and allowed to equilibrate to room temperature for 15min. After equilibration, the medium is removed and the cells are washed twice with at room temperature with DPBS. The cells are lysed with 20 µL/well 1× Passive Lysis Buffer and shaken for 20min at room temperature. Luciferase activity is recorded using an Luminometer Microplate Reader[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [3]
Rats[3]
The effects of increasing doses of L-kynurenine with or without probenecid on concentrations of kynurenic acid in cerebral cortex are examined in 7-day-old rats. Six animals are examined in each group. Animals are treated with L-kynurenine at doses of 100, 200, 300, and 400 mg/kg or kynurenine, 200 mg/kg with probenecid, 50 mg/kg. Animals are killed at 1 h, the brains promptly removed, and the cerebral cortex is dissected 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 a fluorometric assay[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Moyer BJ, et al. Inhibition of the aryl hydrocarbon receptor prevents Western diet-induced obesity. Model for AHR activation by kynurenine via oxidized-LDL, TLR2/4, TGFβ, 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 Flow Metab. 1992 May;12(3):400-7.
D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR)[1][2][3][4].
IC50 & Target[1]
Human Endogenous Metabolite
体外研究 (In Vitro)
D-kynurenine (10, 40, 60, and 100 µM) positively regulates the metastasis of 95D cells, a lung cancer cell line, which is reduced upon siRNAAhr treatment. Significant enhancement VIM expression was detected in the presence of D-kynurenine (10 and 40 µM). 10 µM D-kynurenine markedly attenuates E-cadherin level. 10 µM D-kynurenine-mediated changes of VIM and E-cadherin are substantially attenuated on siRNAAhr treatment as well. The evidences-10/40 µM D-kynurenine-induced up-regulation of CYP1A1, 10 µM D-kynurenine-induced increase of nuclear transfer of Ahr, and 10/40/60/100 µM D-kynurenine-induced enhancement of DER-luciferase activity-indicated that D-kynurenine Is capable of activating Ahr in fact[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
208.21
Formula
C10H12N2O3
CAS 号
13441-51-5
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
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
H2O : 5 mg/mL (24.01 mM; ultrasonic and warming and heat to 60°C)
[1]. Wang XD, et al. A method for the determination of D-kynurenine in biological tissues. Anal Bioanal Chem. 2013 Dec;405(30):9747-54.
[2]. Irukayama-Tomobe Y, et al. Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B. Proc Natl Acad Sci U S A. 2009 Mar 10;106(10):3930-4.
[3]. Kozaki A, et al. Fluorimetric assay for D-amino acid oxidase activity in rat brain homogenate by using D-kynurenine as a substrate. Biosci Trends. 2012 Oct;6(5):241-7.
[4]. Duan Z, et al. Promoting epithelial-to-mesenchymal transition by D-kynurenine via activating aryl hydrocarbon receptor. Mol Cell Biochem. 2018 Nov;448(1-2):165-173.
L-Kynurenine-d4 is the deuterium labeled L-Kynurenine. L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist[1][2].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
212.24
Formula
C10H8D4N2O3
CAS 号
2672568-86-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Moyer BJ, et al. Inhibition of the aryl hydrocarbon receptor prevents Western diet-induced obesity. Model for AHR activation by kynurenine via oxidized-LDL, TLR2/4, TGFβ, and IDO1. Toxicol Appl Pharmacol. 2016 Jun 1;300:13-24.
[3]. 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.
[4]. Nozaki K, et al. Neuroprotective effects of L-kynurenine on hypoxia-ischemia and NMDA lesions in neonatal rats. J Cereb Blood Flow Metab. 1992 May;12(3):400-7.