Cat. No.: HY-N0757

8-O-Acetylharpagide

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

8-O-Acetylharpagide is an orally active iridoid glycoside compound. 8-O-Acetylharpagide exhibits anti-aging activity at low doses and anticancer activity at high doses. 8-O-Acetylharpagide induces late-stage apoptosis and necrosis-like death in cancer cells, and downregulates anti-apoptotic proteins such as Akt, p-Akt and Bcl-2. 8-O-Acetylharpagide is mainly metabolized in rats via demethylation, hydrolysis and glucuronidation, and its active metabolites downregulate the AKT/NF-κB/MMP9 signaling axis. 8-O-Acetylharpagide exerts vasoconstrictive effects by activating vascular α-adrenoceptor.

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

Purity: 99.75%
CAS No.: 6926-14-3
Formula: C₁₇H₂₆O₁₁
Molecular Weight:406.38

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

8-O-Acetylharpagide Chemical Structure

CAS No.: 6926-14-3

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Akt Isoforms :

All Bcl-2 Family Isoforms :

All Adrenergic Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	ED₅₀	310 μM Compound: 2	Cytotoxicity against human A431 cells by MTT assay Cytotoxicity against human A431 cells by MTT assay	[PMID: 12027771]

In Vitro

8-O-acetylharpagide (0.5-10 μM; 48 h) dose-dependently inhibits the activity of senescence-associated β-galactosidase in senescent human dermal fibroblasts in vitro^[1].
8-O-acetylharpagide (0.5-10 μM; 48 h) dose-dependently inhibits p53 expression in senescent human dermal fibroblasts^[1].
8-O-acetylharpagide (1-10 μM) inhibits the elevated intracellular reactive oxygen species levels in dermal fibroblasts from elderly humans^[1].
8-O-acetylharpagide (2.5 mg/mL; 0-24 h) undergoes metabolic transformation in an in vitro rat intestinal flora culture system, producing 2 metabolites via pathways including hydrolysis, reduction and glucuronidation^[2].
8-O-acetylharpagide (0.01-1 mM; 24 h) exhibits more potent selective cytotoxicity against human hypopharyngeal carcinoma FaDu cells than against normal human PDL cells, with an IC₅₀ of 0.88 mM for FaDu cells and 1.65 mM for PDL cells after 24 h of treatment^[3].
8-O-acetylharpagide (1 mM; 24 h) induces significant cell rounding in human hypopharyngeal carcinoma FaDu cells, but exerts no such effect in normal human PDL cells^[3].
8-O-acetylharpagide (1 mM; 6 days) completely inhibits the proliferation of human hypopharyngeal carcinoma FaDu cells^[3].
8-O-acetylharpagide (0.5-1 mM; 24 h) induces dose-dependent G2/M phase arrest in human hypopharyngeal carcinoma FaDu cells and regulates the expression of cell cycle-related proteins, but exerts no effect on the cell cycle distribution of normal human PDL cells^[3].
8-O-acetylharpagide (1 mM; 24 h) induces significant necroptotic cell death and late apoptosis in human hypopharyngeal carcinoma FaDu cells, downregulates anti-apoptotic proteins, but exerts minimal effects on normal human PDL cells^[3].
8-O-acetylharpagide (1 mM; 24 h) significantly enhances the radiosensitivity of human hypopharyngeal carcinoma FaDu cells, but has no effect on that of normal human PDL cells^[3].

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

Western Blot Analysis^[1]

Cell Line:

old human dermal fibroblasts (HDFs)
Concentration:

0.5 μM, 1 μM, 5 μM, 10 μM
Incubation Time:

48 h
Result:

Reduced p53 expression to ~90% of control at 0.5 μM.
Reduced p53 expression to ~75% of control at 1 μM.
Reduced p53 expression to ~60% of control at 5 μM.
Reduced p53 expression to ~55% of control at 10 μM, all in a dose-dependent manner.

Cell Cytotoxicity Assay^[3]

Cell Line:

human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration:

0.01, 0.1, 0.3, 0.5, 0.7, 1 mM
Incubation Time:

24 h
Result:

Reduced viability of FaDu cells significantly at concentrations ≥ 0.5 mM, with an IC₅₀ of 0.88 mM.
Reached an IC₅₀ of 1.65 mM in PDL cells, yielding a selectivity index of ≈1.85.
Enhanced PDL cell viability at low concentrations.

Cell Proliferation Assay^[3]

Cell Line:

human hypopharyngeal cancer FaDu cells
Concentration:

1 mM
Incubation Time:

6 days
Result:

Completely suppressed the proliferation of FaDu cells over the 6-day period, while vehicle-treated cells showed continuous growth.

Cell Cycle Analysis^[3]

Cell Line:

human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration:

0.5, 1 mM
Incubation Time:

24 h
Result:

Induced dramatic G2/M phase arrest and an increased sub-G1 population in FaDu cells treated with 1 mM, with a dose-dependent effect from 0.5-1 mM.
Upregulated CHK1 (1.32-fold), Cyclin B (1.3-fold), and p21 (1.74-fold), and downregulated CDK1 (0.58-fold) relative to GAPDH in FaDu cells.
Showed no significant changes in cell cycle distribution or cell cycle-related protein expression in PDL cells at the same concentrations.

Apoptosis Analysis^[3]

Cell Line:

human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration:

1 mM
Incubation Time:

24 h
Result:

Induced a significant increase in necrosis-like cell population and late apoptosis, with no significant change in early apoptosis in FaDu cells.
Downregulated AKT (0.56-fold), phospho-AKT (0.64-fold), and BCL-2 (0.7-fold) relative to GAPDH in FaDu cells.
Caused only a small increase in necrosis-like cells and no significant changes in apoptosis or apoptosis-related protein expression in PDL cells.

Cell Cytotoxicity Assay^[3]

Cell Line:

human hypopharyngeal cancer FaDu cells, human periodontal ligament (PDL) normal cells
Concentration:

1 mM
Incubation Time:

24 h (pre-incubation); 48 h (post-irradiation incubation)
Result:

Enhanced the radiosensitivity of FaDu cells significantly, with cell viability decreasing more sharply with increasing radiation dose compared to vehicle-treated FaDu cells.
Showed no enhancement of radiosensitivity in PDL cells.

In Vivo

8-O-acetylharpagide (75-150 mg/kg; p.o.; once daily; for 4 consecutive weeks) significantly inhibits the AKT/NF-κB/MMP9 signaling axis in 4T1 breast cancer-bearing Balb-C mice^[2].
8-O-acetylharpagide (low dose; p.o.) inhibits senescent phenotypes in aged mice^[3].

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

Animal Model:

Balb-C (female, 4 weeks old, weight 22 g, subcutaneous injection of 4T1 cells)^[2]
Dosage:

75 mg/kg; 150 mg/kg
Administration:

p.o.; once daily; 4 weeks
Result:

Significantly reduced relative protein levels of AKT, p-AKT, NF-κB p65, and MMP9 compared to the control group.
Significantly reduced the p-AKT/AKT ratio compared to the control group.
Further significantly reduced relative protein levels of AKT, p-AKT, NF-κB p65, and MMP9 compared to the control group.

Chemical Information

CAS No. 6926-14-3
Appearance Solid
Molecular Weight 406.38
Formula C₁₇H₂₆O₁₁
Color White to off-white
SMILES

O[C@@]([C@@H]1O)(C=CO2)[C@]([C@](OC(C)=O)(C)C1)([H])[C@@H]2O[C@]([C@@H]([C@@H](O)[C@@H]3O)O)([H])O[C@@H]3CO
Structure Classification
- Terpenoids
- Iridoids
Initial Source
- Plants
- other families
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (61.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4608 mL

12.3038 mL

24.6075 mL

5 mM

0.4922 mL

2.4608 mL

4.9215 mL

10 mM

0.2461 mL

1.2304 mL

2.4608 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Dilution Calculator

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Hsu WH, et al. Involvement of 8-O-acetylharpagide for Ajuga taiwanensis mediated suppression of senescent phenotypes in human dermal fibroblasts. Sci Rep. 2020;10(1):19731. Published 2020 Nov 12. [Content Brief]

[2]. Zhao X, et al. Metabolism and Excretion of 8-O-Acetylharpagide in Rats and Identification of Its Potential Anti-Breast Cancer Active Metabolites. Drug Des Devel Ther. 2025;19:2795-2815. Published 2025 Apr 10. [Content Brief]

[3]. Yang WY, et al. 8-O-acetylharpagide, an active compound isolated from A. taiwanensis selectively induced G2/M phase arrest and radiosensitivity in hypopharyngeal cancer cells. Biochem Biophys Rep. 2026;45:102431. Published 2026 Jan 6. [Content Brief]

[4]. Breschi MC, et al. Vasoconstrictor activity of 8-O-acetylharpagide from Ajuga reptans. J Nat Prod. 1992;55(8):1145-1148. [Content Brief]

[5]. Hsu WH, et al. Author Correction: Involvement of 8-O-acetylharpagide for Ajuga taiwanensis mediated suppression of senescent phenotypes in human dermal fibroblasts. Sci Rep. 2025 Feb 19;15(1):6080.
[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4608 mL	12.3038 mL	24.6075 mL	61.5188 mL
	5 mM	0.4922 mL	2.4608 mL	4.9215 mL	12.3038 mL
	10 mM	0.2461 mL	1.2304 mL	2.4608 mL	6.1519 mL
	15 mM	0.1641 mL	0.8203 mL	1.6405 mL	4.1013 mL
	20 mM	0.1230 mL	0.6152 mL	1.2304 mL	3.0759 mL
	25 mM	0.0984 mL	0.4922 mL	0.9843 mL	2.4608 mL
	30 mM	0.0820 mL	0.4101 mL	0.8203 mL	2.0506 mL
	40 mM	0.0615 mL	0.3076 mL	0.6152 mL	1.5380 mL
	50 mM	0.0492 mL	0.2461 mL	0.4922 mL	1.2304 mL
	60 mM	0.0410 mL	0.2051 mL	0.4101 mL	1.0253 mL

Keywords

8-O-Acetylharpagide

1 Cited Publications

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8-​O-​Acetylharpagide

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Solvent & Solubility

8-O-Acetylharpagide

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