2. Metabolic Enzyme/Protease Anti-infection
  3. Cytochrome P450 HCV
  4. Gentiopicroside

Gentiopicroside  (Synonyms: Gentiopicrin)

Cat. No.: HY-N0494 Purity: 99.59%
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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.

Gentiopicroside Chemical Structure

Gentiopicroside Chemical Structure

CAS No. : 20831-76-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 44 In-stock
Solution
10 mM * 1 mL in DMSO USD 44 In-stock
Solid
5 mg USD 40 In-stock
10 mg USD 70 In-stock
25 mg USD 130 In-stock
50 mg USD 210 In-stock
100 mg USD 340 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Gentiopicroside Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Gentiopicroside

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

CYP2

 

In Vitro

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.

Gentiopicroside Related Antibodies
In Vivo

Gentiopicroside (20, 40, and 80 mg/kg, p.o.) significantly reduces gastric ulcerindex in mice. Gentiopicroside (20, 40, and 80 mg/kg) also ovbiously decreases the levels of HSP-70, TNF-α, IL-6, MDA and increases ncreased GSH level and SOD activity. In addition, Gentiopicroside normalizes EGF and VEGF level in mice[2].

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

356.32

Formula

C16H20O9
CAS No.
Appearance

Solid

Color

White to off-white

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
Structure Classification
Initial Source
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
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8065 mL 14.0323 mL 28.0647 mL
5 mM 0.5613 mL 2.8065 mL 5.6129 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (280.65 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
Cell Assay
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

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].

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

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
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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Gentiopicroside Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gentiopicroside20831-76-9GentiopicrinCytochrome P450HCVCYPsHepatitis C virusInhibitorinhibitorinhibit

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