Cat. No.: HY-N0914

Ajugol

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.61%
CAS No.: 52949-83-4
Formula: C₁₅H₂₄O₉
Molecular Weight:348.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Ajugol Chemical Structure

CAS No.: 52949-83-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Trypanosoma

All Parasite Isoforms :

All Interleukin Related Isoforms :

All mTOR Isoforms :

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]

In Vitro

Ajugol has antiprotozoal activity against Trypanosoma b. rhodesiense (IC₅₀: 31.8 μg/ml) and Trypanosoma b. rhodesiense (IC₅₀: 7.2 μg/ml)^[1].
Ajugol (0-100 μM, 0-72 h) in tert-butyl hydroperoxide (TBHP)-induced mouse primary chondrocytes restores TBHP-induced proliferation restriction and reduces chondrocyte apoptosis, ECM degradation and ROS accumulation without cytotoxicity (≤50 μM)^[2].
Ajugol (50 μM) in Palmitate (HY-N0830)-induced mouse hepatocytes significantly reduces cellular triglyceride (TG) and total cholesterol (TC) content and plays a protective role in Palmitate-induced lipid accumulation without cytotoxicity^[3].
Ajugol (25,50 μM) activates TFEB-mediated autophagy and promotes TFEB nuclear translocation by regulating mTOR dephosphorylation, enhancing lysosomal biogenesis, alleviating endoplasmic reticulum (ER) stress and lipid degradation in TBHP-induced mouse primary chondrocytes and Alpha Mouse Liver-12 (AML12) cells^[2]^[3].
Ajugol attenuates its protective effects against lipid accumulation and ER stress and ECM after autophagy is blocked by Chloroquine (HY-17589A), indicating that it is dependent on the autophagy pathway to exert its effects^[2]^[3].

MedChemExpress (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.

Parmacokinetics

Species	Dose	Route	AUC	MRT	T_1/2	Clearance (CL)
Rat^[4]	2 mg/kg	i.v.	5743.547 mg·h/L	0.804 h	0.746 h	0.354 L/h/kg

In Vivo

Ajugol (25,50 mg/kg, i.p., once a day, 8 weeks) activates TFEB in vivo and improves the progression of osteoarthritis after DDM (Destabilization of the Medial Meniscus) surgery in an osteoarthritis mouse model^[2].
Ajugol (50 mg/kg, p.o., 12 weeks) improves HFD-induced hepatic steatosis and lipid metabolism disorders by promoting autophagic flux in a high-fat diet (HFD)-fed mouse model^[3].

MedChemExpress (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.

Chemical Information

CAS No. 52949-83-4
Appearance Solid
Molecular Weight 348.35
Formula C₁₅H₂₄O₉
Color White to off-white
SMILES

O[C@H]1[C@](O[C@H](CO)[C@@H](O)[C@@H]1O)([H])O[C@H](OC=C2)[C@@]3([H])[C@]2([H])[C@H](O)C[C@@]3(O)C
Structure Classification
- Terpenoids
- Iridoids
Initial Source
- Plants
- Labiatae
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (3)

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Chin Med

Ajugol's upregulation of TFEB-mediated autophagy alleviates endoplasmic reticulum stress in chondrocytes and retards osteoarthritis progression in a mouse model. [Abstract]

2023 Sep 7;18(1):113. PMID: 37679844
J Ethnopharmacol

Radix Rehmanniae Praeparata promoted zebrafish fin regeneration through aryl hydrocarbon receptor-dependent autophagy. [Abstract]

2024 Sep 15:331:118272. PMID: 38710459
Neuropharmacology

Ajugol ameliorates mitochondrial dysfunction and cognitive decline in Alzheimer's Disease via BNIP3-dependent mitophagy. [Abstract]

2026 Jun 15:291:110923. PMID: 41819485

Solvent & Solubility

In Vitro:

DMSO : ≥ 3.7 mg/mL (10.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8707 mL

14.3534 mL

28.7068 mL

5 mM

0.5741 mL

2.8707 mL

5.7414 mL

10 mM

0.2871 mL

1.4353 mL

2.8707 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deniz Tasdemir, et al. Anti-protozoal and plasmodial FabI enzyme inhibiting metabolites of Scrophularia lepidota roots. Phytochemistry. 2005 Feb;66(3):355-62. [Content Brief]

[2]. Wu J, et al. Ajugol's upregulation of TFEB-mediated autophagy alleviates endoplasmic reticulum stress in chondrocytes and retards osteoarthritis progression in a mouse model. Chin Med. 2023 Sep 7;18(1):113. [Content Brief]

[3]. Zhang H, et al. Ajugol enhances TFEB-mediated lysosome biogenesis and lipophagy to alleviate non-alcoholic fatty liver disease. Pharmacol Res. 2021 Dec;174:105964. [Content Brief]

[4]. Yi L, et al.A novel iridoid glycoside leonuride (ajugol) attenuates airway inflammation and remodeling through inhibiting type-2 high cytokine/chemokine activity in OVA-induced asthmatic mice. Phytomedicine. 2022 Oct;105:154345. [Content Brief]

[5]. Xue B, et al. Pharmacokinetics and tissue distribution of Aucubin, Ajugol and Catalpol in rats using a validated simultaneous LC-ESI-MS/MS assay. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:245-53. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

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Ajugol

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Publications Citing Use of MedChemExpress (MCE) Ajugol

All Parasite Isoforms

All Interleukin Related Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs