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Protopine ADC Cytotoxin inhibitor

Name: Protopine
Brand: Selleck Chemicals
SKU: S3883
Rating: 5 (1 reviews)

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 Channel 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.

Chemical Structure

Molecular Weight: 353.37

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.79

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase
Other ADC Cytotoxin Inhibitors	Triptolide SN-38 Luteolin (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Harmine hydrochloride Luteoloside

Chemical Information, Storage & Stability

Molecular Weight	353.37	Formula	C₂₀H₁₉NO₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	130-86-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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. 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. This chemical inhibits serotonin and noradrenaline Transmembrane Transporters 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.
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. It may be a potential therapeutic agent of antidepressant which targeted on SERT and NET in mice models. It has an antidepressant-like effect on animal models.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21419197/ [2] https://pubmed.ncbi.nlm.nih.gov/22033245/ [3] https://pubmed.ncbi.nlm.nih.gov/16530230/

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