Home Transmembrane Transporters ADC Cytotoxin inhibitor - Calcium Channel inhibitor Protopine For research use only.

Protopine

Synonyms: Corydinine, Fumarine, Biflorine, Macleyine

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.

Protopine Chemical Structure

Protopine Chemical Structure

CAS: 130-86-9

Purity & Quality Control

Batch: S388301 DMSO] 30 mg/mL] false] ] ] false] ] ] false Purity: 99.79%
99.79

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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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Male BALB/cj mice
Dosages 5, 10, 20 mg/kg
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 353.37 Formula

C20H19NO5
CAS No. 130-86-9 SDF Download Protopine SDF
Smiles CN1CCC2=CC3=C(C=C2C(=O)CC4=C(C1)C5=C(C=C4)OCO5)OCO3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 30 mg/mL ( (84.89 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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