Home Metabolism P450 (e.g. CYP17) inhibitor Gentiopicroside For research use only.

Gentiopicroside

Synonyms: Gentiopicrin

Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.

Gentiopicroside Chemical Structure

Gentiopicroside Chemical Structure

CAS No. 20831-76-9

Purity & Quality Control

Gentiopicroside Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Biological Activity

Description Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
Targets
CYP2A6 [1]
(in human liver microsomes)		 CYP2E1 [1]
(in human liver microsomes)
In vitro
In vitro Gentiopicroside (GE) is a non-competitive inhibitor of CYP2A6 at lower concentrations and a competitive inhibitor at higher concentrations. Gentiopicroside does not produce inhibition of CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities. However, a significant increase of CYP1A2 and CYP3A4 activity is observed at high concentrations. In cultured human hepatocytes no significant induction of CYP1A2, CYP3A4 or CYP2B6 is observed[1].
In Vivo
In vivo Gentiopicroside (GE) has a low bioavailability (%F) after oral administration, which may be attributed to the first-pass metabolism in the gut wall or liver, metabolism or decomposition in the intestine by bacterial microflora, and/or poor absorption from the gastrointestinal tract. The Phase I clinical study shows that after intravenous infusion of 80, 240, and 400 mg GE, the mean Cmax are 3.501±0.566 μg/ml, 9.865±1.237 μg/ml, and 16.95±2.571 μg/ml, respectively[1]. GPS can act as hepatoprotective, cholagogic, anti-inflammatory, and antibacterial agents[2].
Animal Research Animal Models Wistar rats
Dosages 200 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 356.32 Formula

C16H20O9
CAS No. 20831-76-9 SDF Download Gentiopicroside SDF
Smiles C=CC1C(OC=C2C1=CCOC2=O)OC3C(C(C(C(O3)CO)O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (199.25 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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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 ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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