Referencia número: HY-N0010

Geniposidic acid

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis.

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Pureza: 98.87%
No. CAS: 27741-01-1
Fòrmula: C₁₆H₂₂O₁₀
Peso molecular:374.34

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Geniposidic acid Chemical Structure

No. CAS: 27741-01-1

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Top Publications Citing

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Fluorescent Dye

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

SIRT6

6.751 × 10 μM (Kd)

Ver todos los productos específicos de isoformas Sirtuin :

Ver todos los productos específicos de isoformas TNF Receptor :

Ver todos los productos específicos de isoformas Interleukin Related :

In Vitro

Geniposidic acid (25-100 μM; 12 h) activates the nuclear translocation of farnesoid X receptor (FXR) in TP-injured human L02 hepatocytes, upregulates key bile acid synthases and transporters to reduce lipid accumulation, and this activity is absolutely dependent on the expression of FXR^[1].
Geniposidic acid directly binds to the ligand-binding domain of human FXR, with a K_d value of 3.905 × 10⁻⁷ M. It binds to FXR in a dose-dependent manner, with an EC₅₀ of 1.076×10^-8 M^[1].
Geniposidic acid (25-100 μM; 24 h) activates BSEP-mediated transcription of BSEP target genes in human L02 hepatocytes, with Ser332 and His447 residues being critical for this agonist activity^[1].
Geniposidic acid (25-100 μM; 72 h) upregulates the expression and nuclear translocation of miR-19a-3p in TP-damaged human L02 hepatocytes via an FXR-dependent mechanism; miR-19a-3p does not regulate FXR expression, but inhibits LXR-mediated cholesterol synthesis, thereby reducing the expression of cholesterol synthesis genes and lipid droplet accumulation^[1].
Geniposidic acid (25-100 μM) reduces OA/PA-induced lipid accumulation and oxidative stress in primary hepatocytes from wild-type mice in a concentration-dependent manner, which depends on functionally intact SIRT6^[3].
Geniposidic acid (25-100 μM) upregulates the expression and deacetylase activity of SIRT6 in HepG2 cells and mouse primary hepatocytes under both normal and lipotoxic conditions^[3].
Geniposidic acid (0.625-80 μM) binds directly to recombinant human SIRT6, with a K_d value of 6.751 × 10⁻⁸ M^[3].
Geniposidic acid (100 μM) reduces OA+PA-induced lipid accumulation in primary hepatocytes from wild-type mice^[3].
Geniposidic acid (100 μM) upregulates the expression of fatty acid oxidation-related genes *Pparα*, *Cpt1α* and *Cd36* in primary hepatocytes from wild-type mice under lipotoxic conditions^[3].

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

Western Blot Analysis^[1]

Cell Line:

L02 cells treatment with TP
Concentration:

25, 50, 100 μM
Incubation Time:

12 h
Result:

restored the protein levels of CYP7A1, CYP7B1, CYP8B1, CYP27A1, and the transporters BSEP, MRP2, and NTCP, which were downregulated in TP-induced liver cell in-jury.

RT-PCR^[1]

Cell Line:

L02 cells treatment with TP
Concentration:

25, 50, 100 μM
Incubation Time:

12 h
Result:

Restored the mRNA levels of CYP7A1, CYP7B1, CYP8B1, CYP27A1, and the transporters BSEP, MRP2, and NTCP, which were downregulated in TP-induced liver cell in-jury.
Activated the expression of mdr2, an FXR target gene.

In Vivo

Geniposidic acid (25-100 mg/kg; i.g.; daily; 6-21 days) in Acetaminophen (HY-66005) and Triptolide (HY-32735) induced liver injury (DILI) mouse models can alleviate liver injury, inflammatory response and bile acid/cholesterol metabolic dysfunction in a concentration-dependent manner by upregulating bile acid synthesis and transport mediators and inhibiting miR-19a-3p-mediated cholesterol synthesis^[1].
Geniposidic acid (25-75 mg/kg; i.g.; daily; 7 days) showed a dose-dependent alleviating effect on DSS-induced colitis in male C57BL/6 mice, including reducing disease activity, restoring colon length, improving colonic tissue morphology, inhibiting the production of pro-inflammatory cytokines, inhibiting NF-κB activation, enhancing the expression of intestinal tight junction proteins, and restoring gut microbiota composition^[2].
Geniposidic acid (75 mg/kg; i.g.; daily; 7 days) showed no visible adverse effects in healthy male C57BL/6 mice and was able to regulate gut microbiota composition^[2].
Geniposidic acid (25-100 mg/kg; i.g.; daily; 4-8 weeks) dose-dependently alleviated metabolic dysfunction-related fatty liver disease induced by high-fat diet (HFD) and MCD in male C57BL/6J mice, with its action dependent on functional liver function^[3].

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

Animal Model:

C57BL/6 (male, 6-8 weeks old, Acetaminophen/Triptolide-induced acute DILI model)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

i.g.; daily; 6 days
Result:

Prevented weight loss caused by acute drug-induced liver injury (DILI).
Reduced acetaminophen-induced increase in liver weight ratio.
Reduced elevated serum ALT and AST levels without affecting ALP levels.
Reduced inflammatory infiltration, hepatocellular necrosis, and F4/80-positive Kupffer cells.
Reduced mRNA levels of hepatic pro-inflammatory cytokines TNF-α, IL-1β, and IL-6, and increases mRNA levels of the anti-inflammatory cytokine IL-10.
Reduced elevated serum and hepatic levels of total bile acids (TBA), total triglycerides (TG), and total cholesterol (TCHO), and reduces hepatic lipid deposition.
Dose-dependently upregulated the mRNA and protein expression of bile acid synthases (CYP7A1, CYP7B1, CYP8B1, CYP27A1) and bile acid transporters (BSEP, MRP2, NTCP) in the liver.

Animal Model:

C57BL/6 (male, 7-8 weeks old, 21-23 g, DSS-induced colitis model)^[2]
Dosage:

25 mg/kg; 50 mg/kg; 75 mg/kg
Administration:

i.g.; daily; 7 days
Result:

Reduced Disease Activity Index (DAI) score and colonic histological damage score.
Increased colonic length.
Decreased colonic TNF-α and IL-1β levels, and NF-κB p65 protein expression.
Upregulated the protein expression of tight junction proteins ZO-1 and occludin in colonic tissue.
Increased the richness and diversity of gut microbiota (Chao1, Shannon, Simpson indices), increases the relative abundance of Bacteroides, and decreases the relative abundance of Verrucous microbes.

Animal Model:

C57BL/6 (male, 7-8 weeks old, 21-23 g)^[2]
Dosage:

75 mg/kg
Administration:

i.g.; daily; 7 days
Result:

Altered the gut microbiota structure, increasing the relative abundance of Proteobacteria, Muribacaceae, Lactobacillus, Verrucomicrobiales, and Akkermansia, while decreasing the relative abundance of Verrucomicrobiota.

Animal Model:

C57BL/6J (male, 8 weeks old, 20±2 g, HFD/MCD-induced)^[3]
Dosage:

25 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

p.o.; daily; 4-8 weeks
Result:

Reduced weight gain and liver weight increase.
Decreased serum ALT, AST, TC, TG, NEFA, and LDL-C levels while increasing serum HDL-C levels.
Reduced macrovesicular steatosis (HE staining) and neutral lipid deposition (Oil Red O staining) in liver sections.
Upregulated the mRNA expression of hepatic fatty acid β-oxidation regulators (Pparα, Cpt1α, Acad1, Acadm).
Increased serum GSH-PX and SOD activities and decreased MDA levels, thereby restoring redox homeostasis.
Reduced fasting blood glucose, improved glucose tolerance and insulin sensitivity, and reduced perirenal fat mass and adipocyte volume.
Reduced F4/80⁺ macrophage infiltration in liver tissue.
Downregulated the hepatic mRNA expression of pro-inflammatory genes (IL-1β, Ccl2, CXcl1) and fibrosis genes (TGF-β, Fn1, Col1a1).
Reduce liver collagen deposition (Masson trichrome staining, Sirius red staining).

Chemical Information

No. CAS 27741-01-1
Appearance Solid
Peso molecular 374.34
Fòrmula C₁₆H₂₂O₁₀
Color White to off-white
SMILES

O[C@H]1[C@H](O)[C@@H](CO)O[C@@H](O[C@@H]2OC=C(C(O)=O)[C@]3([H])[C@@]2([H])C(CO)=CC3)[C@@H]1O
Structure Classification
- Terpenoids
- Iridoids
Initial Source
- Plants
- other families
- Endogenous metabolite
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All Cell Imaging/StainingCell Proliferation/Viability AssayIFWB

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Journal Impact Factor

Phytomedicine

A novel mechanism of Reduning injection in sepsis treatment: Targeting inflammatory kinases TBK1 and IKKβ. [Abstract]

2026 Feb:151:157776. PMID: 41512388
Molecules

Geniposidic Acid from Eucommia ulmoides Oliver Staminate Flower Tea Mitigates Cellular Oxidative Stress via Activating AKT/NRF2 Signaling. [Abstract]

2022 Dec 5;27(23):8568. PMID: 36500666

Geniposidic acid purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Dec 5;27(23):8568. [Abstract]

HaCaT cells were treated with GPA (50 μM) for 24 h before being exposed to H2O2 with indicated concentrations (250 μM, 500 μM, 750 μM) for 4 h. Clonogenic surviving assay was used to evaluate the effects of GPA pretreatment on clonogenicity under oxidative stress.

Geniposidic acid purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Dec 5;27(23):8568. [Abstract]

Cells were exposed to H2O2 (750 μM) for 4 h after being pretreated with GPA (50 μM) for 24 h. Intracellular ROS generation was measured by a fluorescence microscope using a CM−H2DCFDA probe.

Geniposidic acid purchased from MedChemExpress. Usage Cited in: Molecules. 2022 Dec 5;27(23):8568. [Abstract]

Cells were exposed to H2O2 (750 μM) for 4 h after being pretreated with GPA (10 μM, 25 μM, 50 μM) for 24 h. Western blotting was performed to identify the antioxidative genes expression level.
J Cell Mol Med

Geniposidic acid alleviates osteoarthritis progression through inhibiting inflammation and chondrocytes ferroptosis. [Abstract]

2024 Apr;28(8):e18228. PMID: 38520209

Geniposidic acid purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2024 Apr;28(8):e18228. [Abstract]

Cells were cultured with different concentrations of Geniposidic acid (GPA) (12.5, 25 and 50 μM) for 24 h. The cell viability was determined by CCK8 assay.
Neurotox Res

Tubuloside B Alleviates Aβ25-35 Induced PC12 Cell Injury by Attenuating Pyroptosis, Apoptosis and Excessive Autophagy. [Abstract]

2026 Mar 19;44(2):12. PMID: 41854817
Viruses

Anthraquinone-2-Carboxylic Acid Is a Potential Antiviral Candidate Against Influenza Viruses In Vitro and In Vivo. [Abstract]

2025 Apr 27;17(5):628. PMID: 40431640
Food Chem Toxicol

Mechanisms of LPS-induced toxicity in endothelial cells and the protective role of geniposidic acid. [Abstract]

2025 Apr 25:115488. PMID: 40288513
Research Square Preprint

2021 Feb.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (267.14 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

2.6714 mL

13.3568 mL

26.7137 mL

5 mM

0.5343 mL

2.6714 mL

5.3427 mL

10 mM

0.2671 mL

1.3357 mL

2.6714 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

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: ≥ 3 mg/mL (8.01 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (8.01 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (8.01 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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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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:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (293 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)
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- 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Fan M, et al. Geniposidic Acid Targeting FXR "S332 and H447" Mediated Conformational Change to Upregulate CYPs and miR-19a-3p to Ameliorate Drug-Induced Liver Injury. Adv Sci (Weinh). 2025;12(15):e2409107. [Content Brief]

[2]. Jiang P, et al. Geniposidic acid attenuates DSS-induced colitis through inhibiting inflammation and regulating gut microbiota. Phytother Res. 2023;37(8):3453-3466. [Content Brief]

[3]. Zhou Y, et al. Geniposidic acid alleviated metabolic dysfunction-associated steatotic liver disease by exciting SIRT6 signaling. Phytomedicine. 2025;146:157140. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6714 mL	13.3568 mL	26.7137 mL	66.7842 mL
	5 mM	0.5343 mL	2.6714 mL	5.3427 mL	13.3568 mL
	10 mM	0.2671 mL	1.3357 mL	2.6714 mL	6.6784 mL
	15 mM	0.1781 mL	0.8905 mL	1.7809 mL	4.4523 mL
	20 mM	0.1336 mL	0.6678 mL	1.3357 mL	3.3392 mL
	25 mM	0.1069 mL	0.5343 mL	1.0685 mL	2.6714 mL
	30 mM	0.0890 mL	0.4452 mL	0.8905 mL	2.2261 mL
	40 mM	0.0668 mL	0.3339 mL	0.6678 mL	1.6696 mL
	50 mM	0.0534 mL	0.2671 mL	0.5343 mL	1.3357 mL
	60 mM	0.0445 mL	0.2226 mL	0.4452 mL	1.1131 mL
	80 mM	0.0334 mL	0.1670 mL	0.3339 mL	0.8348 mL
	100 mM	0.0267 mL	0.1336 mL	0.2671 mL	0.6678 mL

Keywords

Geniposidic acid

7 Cited Publications

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Geniposidic acid

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Publications Citing Use of MedChemExpress (MCE) Geniposidic acid

Ver todos los productos específicos de isoformas Sirtuin

Ver todos los productos específicos de isoformas TNF Receptor

Ver todos los productos específicos de isoformas Interleukin Related

Actividad biológica

Chemical Information

Publications (7)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Geniposidic acid Related Classifications

HY-N0010 Related Classifications