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  3. Ajugol

Ajugol  (Synonyms: 益母草苷)

目录号: HY-N0914 纯度: 99.13%
COA 产品使用指南 技术支持

Ajugol 是一种从传统中药益母草 (Leonurus japonicus) 中发现的具有口服活性的环烯醚糖苷。Ajugol 是一种自噬 (autophagy) 激活剂。Ajugol 可激活 TFEB 介导的自噬和溶酶体生物合成。Ajugol 还具有抗炎和抗原虫活性作用。Ajugol 在哮喘、非酒精性脂肪肝 (NAFLD)、骨关节炎的疾病研究中具有很大潜力。

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Ajugol

Ajugol Chemical Structure

CAS No. : 52949-83-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1320
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1 mg ¥548
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5 mg ¥1200
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10 mg ¥2000
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Other Forms of Ajugol:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Ajugol is an orally active iridoid glycoside found in the traditional Chinese medicine Leonurus japonicus. Ajugol is an autophagy activator. Ajugol activates TFEB-mediated autophagy and lysosomal biogenesis. Ajugol also has anti-inflammatory effects. Ajugol has great potential in the research of asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis[1][2][3][4].

IC50 & Target

Trypanosoma

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 IC50
> 10 μM
Compound: 11
Cytotoxicity against human A2780 cells by MTT assay
Cytotoxicity against human A2780 cells by MTT assay
[PMID: 26859776]
A549 IC50
> 10 μM
Compound: 11
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 26859776]
Bel-7402 IC50
> 10 μM
Compound: 11
Cytotoxicity against human Bel7402 cells by MTT assay
Cytotoxicity against human Bel7402 cells by MTT assay
[PMID: 26859776]
BGC-823 IC50
> 10 μM
Compound: 11
Cytotoxicity against human BGC823 cells by MTT assay
Cytotoxicity against human BGC823 cells by MTT assay
[PMID: 26859776]
HT-29 IC50
> 10 μM
Compound: 11
Cytotoxicity against human HT-29 cells by MTT assay
Cytotoxicity against human HT-29 cells by MTT assay
[PMID: 26859776]
体外研究
(In Vitro)

Ajugol 具有抗原虫活性,对 Trypanosoma b. rhodesiense (IC50: 31.8 μg/ml),对Trypanosoma b. rhodesiense (IC50: 7.2 μg/ml) [1]
Ajugol (0-100 μM, 0-72 h) 在 tert-butyl hydroperoxide (TBHP) 诱导的小鼠原代软骨细胞中,可恢复 TBHP 诱导的增殖限制和减少软骨细胞凋亡,ECM 降解和 ROS 积累的作用,且无细胞毒性 (≤50 μM)[2]
Ajugol (50 μM) 在 Palmitate (HY-N0830) 诱导的小鼠肝细胞中,可显著降低细胞甘油三酸酯 (TG) 和总胆固醇 (TC) 含量,在 Palmitate 诱导的脂质积累中起保护作用,且无细胞毒性[3]
Ajugol (25,50 μM) 在 TBHP 诱导的小鼠原代软骨细胞和 Alpha Mouse Liver-12 (AML12) 细胞中,激活 TFEB 介导的自噬和通过调节 mTOR 去磷酸化来促进 TFEB 核转位,增强溶酶体生物发生,缓解内质网 (ER) 应激和脂肪降解的作用[2][3]
Ajugol 在被 Chloroquine (HY-17589A) 阻断自噬后,减弱了抗脂质积累和 ER 应激和 ECM 的保护作用,表明其依赖自噬途径发挥作用[2][3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: Primary mouse hepatocytes, AML12 cells
Concentration: 50 μM
Incubation Time: 24 h
Result: Increased LC3-II (an autophagosome marker) and decreased p62 (an autophagy substrate), indicating enhanced autophagic activity.
Increased nuclear TFEB and upregulated expression of lysosome-related proteins (LAMP2, ATP6V1A).
Reduced p-mTOR, p-S6K, and p-4EBP1 levels, indicated that it inhibited mTORC1 activity.
药代动力学
(Parmacokinetics)[4]
Species Dose Route Indicator value
Rat 2 mg/kg i.v. AUC0-t 5743.547 mg·h/L
Rat 2 mg/kg i.v. AUC0-∞ 5747.104 mg·h/L
Rat 2 mg/kg i.v. MRT 0.804 hr
Rat 2 mg/kg i.v. T1/2 0.746 hr
Rat 2 mg/kg i.v. CL 0.354 L/h/kg
体内研究
(In Vivo)

Ajugol (25,50 mg/kg,i.p.,一天一次,8 周) 在骨关节炎小鼠模型中,在体内激活 TFEB,并改善内侧半月板不稳定症手术后骨关节炎的进展[2]
Ajugol (50 mg/kg,p.o.,12 周) 在 high-fat diet (HFD) 喂养的小鼠模型中,促进自噬通量来改善 HFD 诱发的肝脏脂肪变性和脂质代谢紊乱[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (male aged 10 weeks) the osteoarthritis (OA) model was established using the DMM technique[2]
Dosage: 25, 50 mg/kg
Administration: i.p., once a day, 8 weeks
Result: Had a protective effect on the cartilage of knee joint tissue, reduced the expression of TFEB and type II collagen, while increasing the expression of CHOP and ATF4.
Showed good efficacy in delaying OA progression in the DMM mice model.
Animal Model: C57BL/6 mice (male, aged 6 weeks, 20-23 g) fed HFD[3]
Dosage: 50 mg/kg
Administration: p.o. 12 weeks
Result: Lowered blood glucose and improved insulin resistance in HFD-fed obese mice and also prevented HFD-induced liver injury, with significant decreases in serum AST and ALT levels.
Reduced serum TG, LDL-C, TC, FFA and liver FFA levels as well as LDL-C/HDL-C.
Increased LC3-II levels and decreased p62 levels, demonstrated protection against hepatic steatosis by improving autophagic flux.
分子量

348.35

Formula

C15H24O9

CAS 号
性状

固体

颜色

White to off-white

中文名称

益母草苷

结构分类
初始来源
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
细胞实验: 

DMSO 中的溶解度 : ≥ 3.7 mg/mL (10.62 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8707 mL 14.3534 mL 28.7068 mL
5 mM 0.5741 mL 2.8707 mL 5.7414 mL
查看完整储备液配制表

* 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.13%

参考文献

完整储备液配制表

* 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8707 mL 14.3534 mL 28.7068 mL 71.7669 mL
5 mM 0.5741 mL 2.8707 mL 5.7414 mL 14.3534 mL
10 mM 0.2871 mL 1.4353 mL 2.8707 mL 7.1767 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
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