Harpagoside |
Catalog No.GN10620
One-Click Copy Product Info
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Harpagoside is a natural iridoid glycoside with anti-inflammatory, anticancer, and neuroprotective activities.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 19210-12-9
Sample solution is provided at 25 µL, 10mM.
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Harpagoside is a natural iridoid glycoside with anti-inflammatory, anticancer, and neuroprotective activities. Harpagoside inhibits NF-κB and AP-1 activation, downregulates iNOS, COX-2, TNF-α, IL-6, and IL-1β, reduces oxidative stress through the Nrf2/HO-1 axis, and inhibits osteoclast differentiation. Harpagoside can be used for research on osteoarthritis, rheumatoid arthritis, chronic pain, and Alzheimer's disease[1-4].
In vitro, treatment of IFNγ/LPS-stimulated THP-1 cells with 5-500μM Harpagoside for 24 hours reduced TNFα secretion[5]. Pretreatment of HepG2 cells with 200μM Harpagoside for 2 hours followed by 10µg/ml LPS treatment for 1 or 6 hours. Harpagoside inhibited COX-2 and iNOS protein expression, blocked NF-κB p65 nuclear translocation, and inhibited IκB-α degradation[6]. Pretreatment of cultured rat mesencephalic neurons with 1µM Harpagoside for 24 hours followed by 10µM 1-Methyl-4-phenylpyridine treatment for 48 hours. Harpagoside reduced TH-positive neuron loss and axon length shortening[7].
In vivo, oral administration of 10mg/kg Harpagoside to DBA/1 arthritic mice every other day until day 42. Harpagoside reduced arthritis clinical scores, alleviated ankle joint inflammation, cartilage destruction, pannus formation, and local bone erosion, decreased serum TNF-α, IL-6, and IL-1β, downregulated RANKL, upregulated OPG, reduced trabecular bone loss in femur, and decreased TRAP-positive osteoclasts[8]. Epidural injection of 100-200μg/kg Harpagoside to lumbar spinal stenosis rats once daily for 4 weeks. Harpagoside reduced ED1+ inflammatory cell infiltration, decreased iNOS, IL-1β, TNF-α, and COX2 expression, upregulated IL-10 and Arg1, improved gait, motor function, ladder walking performance, and mechanical pain threshold[9]. Oral administration of 42mg/kg Harpagoside to C57BL/6 mice once daily for 4 weeks after 4 weekly tail vein injections of 5mg/kg doxorubicin. Harpagoside improved EF and FS values, alleviated myocardial fiber loss and disarray, reduced serum LDH and CK-MB, decreased cardiomyocyte apoptosis, and reduced mtDNA oxidative damage[10].
References:[1] Kaur H, Kumar D, Gauttam VK, et al. Decoding the mechanistic landscape of harpagoside: From molecular targets to translational pharmacology. Fitoterapia. 2026 Jan;188:107029.
[2] Haseeb A, Ansari MY, Haqqi TM. Harpagoside suppresses IL-6 expression in primary human osteoarthritis chondrocytes. J Orthop Res. 2017 Feb;35(2):311-320.
[3] Pérez Gutiérrez RM, Rodríguez-Serrano LM, Laguna-Chimal JF, et al. Geniposide and Harpagoside Functionalized Cerium Oxide Nanoparticles as a Potential Neuroprotective. Int J Mol Sci. 2024 Apr 11;25(8):4262.
[4] Lang J, Xiong Z. Protective effects of harpagoside on mitochondrial functions in rotenone‑induced cell models of Parkinson's disease. Biomed Rep. 2025 Feb 11;22(4):64.
[5] Schopohl P, Grüneberg P, Melzig M.F, et al. The influence of harpagoside and harpagide on TNFα-secretion and cell adhesion molecule mRNA-expression in IFN/LPS-stimulated THP-1 cells. Fitoterapia. 2016;113:148-156.
[6] Huang T, Tran V, Duke R, et al. Harpagoside suppresses lipopolysaccharide-induced iNOS and COX-2 expression through inhibition of NF-kB activation. Journal of Ethnopharmacology. 2006;104(1-2):149-55.
[7] Sun X, Xiong Z, Zhang Y, et al. Harpagoside attenuates MPTP/MPP+ induced dopaminergic neurodegeneration and movement disorder via elevating glial cell line-derived neurotrophic factor. J Neurochem. 2012;120(6):1072-1083.
[8] Kim J-Y, Cheon Y-H, Ahn S-J, et al. Harpagoside attenuates local bone erosion and systemic osteoporosis in collagen-induced arthritis in mice. BMC Complement Med Ther. 2022;22:214.
[9] Hong J.Y, Kim H, Yeo C, et al. Epidural Injection of Harpagoside for the Recovery of Rats with Lumbar Spinal Stenosis. Cells. 2023;12(18):2281.
[10] Li W, Wang X, Liu T, et al. Harpagoside Protects Against Doxorubicin-Induced Cardiotoxicity via P53-Parkin-Mediated Mitophagy. Front Cell Dev Biol. 2022 Feb 10;10:813370.
| Cell experiment [1]: | |
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Cell lines |
RAW 264.7 cells (mouse macrophage cell line) and HepG2 cells (human hepatocellular carcinoma cell line) |
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Preparation Method |
RAW 264.7 cells were pretreated with Harpagoside at 0.1-200μM for 1 hour prior to 100ng/ml LPS stimulation for 24 hours; supernatant was collected for nitrite assay. RAW 264.7 cells were transfected with pNF-κB-Luc plasmid, pretreated with Harpagoside at 0.1-200μM for 2 hours, then treated with 100ng/ml LPS for 4 hours; cells were lysed for luciferase assay. HepG2 cells were pretreated with 200μM Harpagoside for 2 hours, then exposed to 10μg/ml LPS for 1 or 6 hours; total RNA was extracted for semi-quantitative RT-PCR and protein was extracted for immunoblotting. |
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Reaction Conditions |
0.1-200μM; 1-24h |
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Applications |
Harpagoside inhibited LPS-induced nitric oxide release, inhibited LPS-stimulated NF-κB promoter activity in transfected RAW 264.7 cells. Harpagoside inhibited LPS-induced COX-2 and iNOS mRNA and protein expression, blocked LPS-induced translocation of NF-κB p65 into nuclear compartments and degradation of IκB-α in HepG2 cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 mice |
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Preparation Method |
C57BL/6 mice were injected into the tail vein with DOX (5mg/kg) once weekly for 4 weeks to establish DICT model. One week after the last injection of DOX or saline, mice were orally administered 42mg/kg Harpagoside daily for 4 weeks. Echocardiographic assessment of cardiac functions was performed, and mice were sacrificed for histological examination (H&E staining), TUNEL assay, DHE staining, TEM, immunohistochemistry/immunofluorescence and immunoblot analysis. |
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Dosage form |
42mg/kg; p.o.; daily for 4 weeks |
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Applications |
Harpagoside improved EF and FS values, reduced LVID;d and LVID;s, and thickened LVAW;s and LVPW;s in DICT mice. Harpagoside alleviated myofibrillar loss, disordered arrangement, enlarged intercellular structures and plasma-dissolved cardiomyocytes, reduced serum LDH and CK-MB, reduced apoptosis, decreased p53 and Bax/Bcl-2 ratio, reduced ROS, MDA and increased SOD, reduced mtDNA damage in DICT mice. |
| References: [1] Huang T, Tran V, Duke R, et al. Harpagoside suppresses lipopolysaccharide-induced iNOS and COX-2 expression through inhibition of NF-kB activation. J Ethnopharmacol. 2006;104(1-2):149-55. [2] Li W, Wang X, Liu T, et al. Harpagoside Protects Against Doxorubicin-Induced Cardiotoxicity via P53-Parkin-Mediated Mitophagy. Front Cell Dev Biol. 2022;10:813370. | |
| Cas No. | 19210-12-9 | SDF | |
| Chemical Name | [(1S,4aS,5R,7S,7aS)-4a,5-dihydroxy-7-methyl-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,5,6,7a-tetrahydrocyclopenta[c]pyran-7-yl] (E)-3-phenylprop-2-enoate | ||
| Canonical SMILES | CC1(CC(C2(C1C(OC=C2)OC3C(C(C(C(O3)CO)O)O)O)O)O)OC(=O)C=CC4=CC=CC=C4 | ||
| Formula | C24H30O11 | M.Wt | 494.18 |
| Solubility | ≥ 49.4mg/mL in EtOH | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0236 mL | 10.1178 mL | 20.2355 mL |
| 5 mM | 404.7 μL | 2.0236 mL | 4.0471 mL |
| 10 mM | 202.4 μL | 1.0118 mL | 2.0236 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)