1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Gentiopicroside

Gentiopicroside (Synonyms: Gentiopicrin)

Cat. No.: HY-N0494 Purity: >98.0%
Handling Instructions

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 antianti-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
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
25 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 370 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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 antianti-inflammatoryand antioxidative effects.

IC50 & Target

IC50: 61 µM (CYP2A6)[1]
Ki: 22.8 µM (CYP2A6)[1]

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].

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].

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 : ≥ 150 mg/mL (420.97 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
10 mM 0.2806 mL 1.4032 mL 2.8065 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

356.32

Formula

C₁₆H₂₀O₉

CAS No.

20831-76-9

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

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Gentiopicroside
Cat. No.:
HY-N0494
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Gentiopicroside

Cat. No.: HY-N0494