Protopine

Catalog No.S3883 Batch:S388301

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Technical Data

Formula

C20H19NO5
Molecular Weight 353.37 CAS No. 130-86-9
Solubility (25°C)* In vitro DMSO 30 mg/mL (84.89 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.)

Preparing Stock Solutions

Biological Activity

Description Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
In vitro Protopine is found to be cytoprotective against oxidative stress-induced cell death in vitro. It inhibits several human CYP enzymes and is reported to be potent inhibitors of CYP2D6 and to suppress, albeit with less potency, the activities of CYP3A4, CYP1A2, and CYP2B6 as well. Protopine also inhibits CYP2C19[1]. Protopine is a novel microtubule stabilizer with anticancer activity in HRPC cells through apoptotic pathway by modulating Cdk1 activity and Bcl-2 family of proteins[2]. Protopine inhibits serotonin and noradrenaline transporter with IC50 values of 0.94 and 19.5 μM. The inhibiting effect of protopine on serotonin uptake (Ki = 0.92 μM) is stronger than that of protopine on NE uptake (Ki = 19.26 μM[3].
In vivo A pharmacokinetic study in rats after oral administration of a single dose of Rhizoma Corydalis Decumbentis extract, equivalent to 15.4 mg of protopine per kg of body weight, shows that the maximum plasma level of protopine reaches 348 ng/ml, i.e. 0.98 μM. In a similar study on rabbits, the maximum plasma concentration of protopine is 1.03 g/ml, i.e. 2.91 μM[1]. Protopine may be a potential therapeuticagent of antidepressant which targeted on SERT and NET in mice models. It has an antidepressant-like effect on animal models[3].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    HepG2 cells

  • Concentrations

    1-75 μM

  • Incubation Time

    24 h

  • Method

    The cells are grown in 75cm2 flasks and sub-cultured before confluence. For all experiments, with the exception of gene reporter assays, HepG2 cells (passages 5–15) are seeded in the complete culture medium at a density of 1×105 cells/cm2. After overnight stabilization, cells are treated with the tested alkaloids or 5 nM TCDD (positive control). Negative controls are treated with 0.1% (v/v) DMSO only.
Animal Study:[3]
  • Animal Models

    Male BALB/cj mice

  • Dosages

    5, 10, 20 mg/kg

  • Administration

    i.p.

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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.