牛蒡苷元 /Arctigenin
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货号：A420992
同义名：
牛蒡子苷元
/ (-)-Arctigenin
Arctigenin is a naturally occuring agonist of adiponectin receptor 1 with IC50 value of 2.6μM.
Arctigenin 化学结构
Arctigenin 3D分子结构
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Arctigenin 纯度/质量文件 产品仅供科研
货号：A420992
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Arctigenin 质控信息
Arctigenin 生物活性
描述
Arctigenin is a phenylpropanoid metabolite with antioxidant and anti-inflammatory activities. Arctigenin at 1μM inhibited LPS-induced nuclear NF-κB activation and nuclear translocation of p65, accompanied by inhibition of I-κBα phosphorylation. It inhibited LPS-inducible increase in the iNOS mRNA by 0.01–1μM Arctigenin, with IC50 value<0.01μM for inhibition of the induction of iNOS by LPS[8] [9] [10]
Arctigenin 动物研究
Dose
Piglet: 2 mg/kg[4] [5] [6]
Administration
i.v., p.o., i.p.
Pharmacokinetics
Animal
Rats[7]
Dose
36 mg/kg
Administration
i.g.
Vd
1040 ± 326 L/kg (day 1)
Tmax
0.2 ± 0.15 h (day 1)
CL
643 ± 153 L/h·kg (day 1)
Cmax
29.6 ± 15.3 µg/l (day 1)
MRT0→t
1.71 ± 0.23 h (day 1)
AUC0→∞
75.2 ± 23.5 µg/l·h (day 1)
AUC0→t
48.3 ± 11.2 µg/l·h (day 1)
Arctigenin 参考文献
[1] Cho MK, Park JW, et al. Potent inhibition of lipopolysaccharide-inducible nitric oxide synthase expression by dibenzylbutyrolactone lignans through inhibition of I-kappaBalpha phosphorylation and of p65 nuclear translocation in macrophages. Int Immunopharmacol. 2002 Jan;2(1):105-16.
[2] Sun Y, Zang Z, et al. Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay. PLoS One. 2013 May 14;8(5):e63354.
[3] Jang YP, Kim SR, et al. Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor. J Neurosci Res. 2002 Apr 15;68(2):233-40.
[4] He B, Zhang HJ, et al. Pharmacokinetics of Arctigenin and Fructus Arctii Powder in Piglets. Front Vet Sci. 2019 Jul 25;6:235.
[5] Wang P, Solorzano W, et al. Arctigenin inhibits prostate tumor cell growth in vitro and in vivo. Clin Nutr Exp. 2017 Jun;13:1-11.
[6] Yang J, Yin HS, et al. Arctigenin Attenuates Ischemia/Reperfusion Induced Ventricular Arrhythmias by Decreasing Oxidative Stress in Rats. Cell Physiol Biochem. 2018;49(2):728-742.
[7] Tan YJ, Ren YS, et al. 28-Day Oral Chronic Toxicity Study of Arctigenin in Rats. Front Pharmacol. 2018 Sep 26;9:1077.
[8] Cho MK, Park JW, Jang YP, Kim YC, Kim SG. Potent inhibition of lipopolysaccharide-inducible nitric oxide synthase expression by dibenzylbutyrolactone lignans through inhibition of I-kappaBalpha phosphorylation and of p65 nuclear translocation in macrophages. Int Immunopharmacol. 2002 Jan;2(1):105-16. doi: 10.1016/s1567-5769(01)00153-9. PMID: 11789661.
[9] Sun Y, Zang Z, Zhong L, Wu M, Su Q, Gao X, Zan W, Lin D, Zhao Y, Zhang Z. Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay. PLoS One. 2013 May 14;8(5):e63354. doi: 10.1371/journal.pone.0063354. PMID: 23691032; PMCID: PMC3653934.
[10] Jang YP, Kim SR, Choi YH, Kim J, Kim SG, Markelonis GJ, Oh TH, Kim YC. Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor. J Neurosci Res. 2002 Apr 15;68(2):233-40. doi: 10.1002/jnr.10204. PMID: 11948668.
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Arctigenin 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.69mL
0.54mL
0.27mL
13.43mL
2.69mL
1.34mL
26.85mL
5.37mL
2.69mL
Arctigenin 技术信息
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