Gentiopicroside
Based on 4 publication(s) in Google Scholar
Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 20831-76-9
- Formula: C16H20O9
- Molecular Weight:356.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
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Publications Citing Use of MedChemExpress (MCE) Gentiopicroside
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Customer Validation & Images
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
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WB
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IF
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Histological Imaging/Staining
Biological Activity
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CYP2 |
Gentiopicroside inhibits P450 activity, with an IC50 and a Ki of 61 μM and 8.12 μM for CYP2A6, also slightly inhibits CYP2E1 activity with an IC50 of 1.6 mM, but shows no inhibition on CYP1A2 and CYP3A4[1]. Gentiopicroside (12.5, 25 and 50 μM) inhibits RANKL-induced osteoclast formation from mouse bone marrow macrophages (BMMs) in a dose-dependent manner, blocks the expression of osteoclast-related proteins, prevents receptor activator of nuclear factor-κB ligand (RANKL)-triggered JNK and NF-κB activation. Gentiopicroside (50 μM) also inhibits RANKL-induced bone resorption[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 20831-76-9
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Appearance Solid
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Molecular Weight 356.32
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Formula C16H20O9
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Color White to off-white
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SMILES
C=C[C@@H]([C@@H]1O[C@]([C@@H]([C@@H](O)[C@@H]2O)O)([H])O[C@@H]2CO)C(C3=CO1)=CCOC3=O
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Synonyms
Gentiopicrin
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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J Ethnopharmacol
Gentiopicroside activates PINK1-dependent mitophagy to inhibit ferroptosis and promote flap survival. [Abstract]2026 Jun 12:364:121504. PMID: 41812934
Gentiopicroside purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2026 Jun 12:364:121504. [Abstract]
Both low- and high-dose GPS treatments markedly enhanced migratory capacity in comparison with the control group treated with Gentiopicrosid (50, 100 mg/kg, i.p.).
Gentiopicroside purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2026 Jun 12:364:121504. [Abstract]
The CCK-8 assay confirmed that GPS promoted cell proliferation treated with Gentiopicrosid (50, 100 mg/kg, i.p.).
Gentiopicroside purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2026 Jun 12:364:121504. [Abstract]
Western blotting was used to assess PINK1, Parkin, and LC3B expression in flap tissues treated with Gentiopicrosid (50, 100 mg/kg, i.p.).
Gentiopicroside purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2026 Jun 12:364:121504. [Abstract]
Immunofluorescence detected the expression of LC3 in mitochondria treated with Gentiopicrosid (100 mg/kg, i.p.).
Gentiopicroside purchased from MedChemExpress. Usage Cited in: J Ethnopharmacol. 2026 Jun 12:364:121504. [Abstract]
H&E detected the extent of neutrophil infiltration in flap tissues of rats treated with Gentiopicrosid (50, 100 mg/kg, i.p.).
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Chin J Integr Med
Gentiopicroside Alleviates Atherosclerosis by Suppressing Reactive Oxygen Species-Dependent NLRP3 Inflammasome Activation in Vascular Endothelial Cells via SIRT1/Nrf2 Pathway. [Abstract]2025 Feb;31(2):118-130. PMID: 39671057 -
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
DMSO : 250 mg/mL (701.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (280.65 mM)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (280.65 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Cell viability is evaluated using the CCK-8 assay. In brief, bone marrow macrophages (BMMs) (1 × 104 cells/well) are placed in a 96-well plate and cultured with various concentrations of Gentiopicroside (12.5, 25 and 50 μM) for 48 h in the presence of M-CSF (30 ng/mL) and RANKL (100 ng/mL). Then, 10 μL of the CCK-8 solution is added to each well and the mixture is incubated for 4 h at 37 °C. The absorbance is evaluated at 450 nm using a microplate reader[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Mice are ran-domLy divided into six groups with 10 animals each. Drug is given by intragastric administration once a day for three consecutive days. Mice in the normal control group and the ethanol control group (negative control) receive saline at a dose of 2.5 mL/kg; Mice in the cimetidine control group (positive control) receive cimetidine at a dose of 100 mg/kg; mice in three Gentiopicroside investigative groups receive different doses of Gentiopicroside (20, 40, and 80 mg/kg), respectively; On the third day, except that mice in the normal control group receive saline, mice in other groups receive 70% ethanol at a dose of 0.01 mL/g by oral1 hr after the last intragastric administration. One hour after the induction, animals are euthanized under anesthesia by cervical dislocation, removed and cut the stomach longitudinally. The stomach are opened along the greater curvature and rinsed slightly with ice-cold saline to remove the gastric contents, and then the severity of gastric mucosal injury is evaluated by gastric ulcer index. Subsequently, each animal'sstomach is cut into two moieties, with one moiety of stomach stored at −80°C for biochemical assessment and the other moiety immersed in 4% paraformaldehyde solution for histopathological examinations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Deng Y, et al. In vitro inhibition and induction of human liver cytochrome P450 enzymes by gentiopicroside: potent effect on CYP2A6. Drug Metab Pharmacokinet. 2013;28(4):339-44. Epub 2013 Feb 19. [Content Brief]
[2]. Yang Y, et al. Protective effect of gentiopicroside from Gentiana macrophylla Pall. in ethanol-induced gastric mucosal injury in mice. Phytother Res. 2018 Feb;32(2):259-266. [Content Brief]
[3]. Chen F, et al. Gentiopicroside inhibits RANKL-induced osteoclastogenesis by regulating NF-κB and JNK signaling pathways. Biomed Pharmacother. 2018 Apr;100:142-146. [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.8065 mL | 14.0323 mL | 28.0647 mL | 70.1617 mL |
| 5 mM | 0.5613 mL | 2.8065 mL | 5.6129 mL | 14.0323 mL | |
| 10 mM | 0.2806 mL | 1.4032 mL | 2.8065 mL | 7.0162 mL | |
| 15 mM | 0.1871 mL | 0.9355 mL | 1.8710 mL | 4.6774 mL | |
| 20 mM | 0.1403 mL | 0.7016 mL | 1.4032 mL | 3.5081 mL | |
| 25 mM | 0.1123 mL | 0.5613 mL | 1.1226 mL | 2.8065 mL | |
| 30 mM | 0.0935 mL | 0.4677 mL | 0.9355 mL | 2.3387 mL | |
| 40 mM | 0.0702 mL | 0.3508 mL | 0.7016 mL | 1.7540 mL | |
| 50 mM | 0.0561 mL | 0.2806 mL | 0.5613 mL | 1.4032 mL | |
| 60 mM | 0.0468 mL | 0.2339 mL | 0.4677 mL | 1.1694 mL | |
| 80 mM | 0.0351 mL | 0.1754 mL | 0.3508 mL | 0.8770 mL | |
| 100 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7016 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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