Home Transmembrane Transporters ADC Cytotoxin inhibitor - Calcium Channel inhibitor Protopine

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Protopine ADC Cytotoxin inhibitor

Cat.No.S3883

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 ADC Cytotoxin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 353.37

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 353.37 Formula

C20H19NO5

 Storage (From the date of receipt)
CAS No. 130-86-9 Download SDF Storage of Stock Solutions

Synonyms Corydinine, Fumarine, Biflorine, Macleyine Smiles CN1CCC2=CC3=C(C=C2C(=O)CC4=C(C1)C5=C(C=C4)OCO5)OCO3

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (84.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Mechanism of Action

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. This compound also inhibits CYP2C19[1]. It 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]. This chemical inhibits serotonin and noradrenaline transporter with IC50 values of 0.94 and 19.5 μM. The inhibiting effect of this compound 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 this compound reaches 348 ng/ml, i.e. 0.98 μM. In a similar study on rabbits, the maximum plasma concentration of this chemical is 1.03 g/ml, i.e. 2.91 μM[1]. It 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].
References

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