Home Metabolism P450 (e.g. CYP17) inhibitor Gentiopicroside

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Gentiopicroside P450 (e.g. CYP17) inhibitor

Cat.No.S3777

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 this compound does not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
Gentiopicroside P450 (e.g. CYP17) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 356.32

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Quality Control

Batch: Purity: 99.72%
99.72

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (199.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 356.32 Formula

C16H20O9

 Storage (From the date of receipt)
CAS No. 20831-76-9 Download SDF Storage of Stock Solutions

Synonyms Gentiopicrin Smiles C=CC1C(OC=C2C1=CCOC2=O)OC3C(C(C(C(O3)CO)O)O)O

Mechanism of Action

Targets/IC50/Ki
CYP2A6
(in human liver microsomes)
CYP2E1
(in human liver microsomes)
In vitro
Gentiopicroside (GE) is a non-competitive inhibitor of CYP2A6 at lower concentrations and a competitive inhibitor at higher concentrations. This compound 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.
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 of this compound, the mean Cmax are 3.501±0.566 μg/ml, 9.865±1.237 μg/ml, and 16.95±2.571 μg/ml, respectively. This chemical can act as hepatoprotective, cholagogic, anti-inflammatory, and antibacterial agents.
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