Gentiopicroside

Catalog No.S3777 Batch:S377702

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Technical Data

Formula

C16H20O9

Molecular Weight 356.32 CAS No. 20831-76-9
Solubility (25°C)* In vitro DMSO 71 mg/mL (199.25 mM)
Water 71 mg/mL (199.25 mM)
Ethanol 18 mg/mL (50.51 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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 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].

Protocol (from reference)

Animal Study:[2]
  • Animal Models

    Wistar rats

  • Dosages

    200 mg/kg

  • Administration

    oral administration

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.