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CAS No.: 7770-78-7

牛蒡苷元 Catalog No. CSN16468

Synonyms: (-)-Arctigenin;牛蒡子苷元

Arctigenin is a naturally occuring agonist of adiponectin receptor 1 with IC50 value of 2.6μM.

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靶点选择性

生物活性

实验方案

技术信息

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]. Arctigenin also works as an active adiponectin receptor 1 agonist with IC50 value of 2.6μM for AdipoR1^[9]. Arctigenin exerted significant neuroprotective effects on glutamate-injured primary cultures of rat cortical cells by directly binding to kainic acid receptors and partly scavenging of free radicals^[10].

动物研究

剂量

Piglet: 2 mg/kg^[4] (i.v.); 50 mg/kg - 100 mg/kg^[5] (p.o.) Rat: 12.5 mg/kg - 200 mg/kg^[6] (i.p.)

给药途径

i.v., p.o., i.p.

动物药代数据

Animal	Rats^[7]
Dose	36 mg/kg
Administration	i.g.
V_d	1040 ± 326 L/kg (day 1) 1110 ± 469 L/kg (day 28)
T_max	0.2 ± 0.15 h (day 1) 0.2843 ± 0.172 h (day 28)
CL	643 ± 153 L/h·kg (day 1) 661 ± 294 L/h·kg (day 28)
C_max	29.6 ± 15.3 µg/l (day 1) 40.7 ± 11.7 µg/l (day 28)
MRT_0→t	1.71 ± 0.23 h (day 1) 1.39 ± 0.81 h (day 28)
AUC_0→∞	75.2 ± 23.5 µg/l·h (day 1) 66.1 ± 32.3 µg/l·h (day 28)
AUC_0→t	48.3 ± 11.2 µg/l·h (day 1) 49.7 ± 18.9 µg/l·h (day 28)

临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT03703388 Healthy Phase 1 Not yet recruiting July 15, 2020 -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03703388	Healthy	Phase 1	Not yet recruiting	July 15, 2020	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6852 mL
- 13.4260 mL
- 26.8520 mL
- 5 mM
- 0.5370 mL
- 2.6852 mL
- 5.3704 mL
- 10 mM
- 0.2685 mL
- 1.3426 mL
- 2.6852 mL

技术信息

CAS号

7770-78-7

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H24O6

运输

蓝冰

分子量

372.41

别名

(-)-Arctigenin;牛蒡子苷元

溶解度

DMSO	124.0 mg/mL (333.0 mM)

动物实验配方

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