Name: Maprotiline HCl
Brand: Selleck Chemicals
SKU: S2517
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (197.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 52 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
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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%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	313.86	Formula	C₂₀H₂₃N.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	10347-81-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CNCCCC12CCC(C3=CC=CC=C31)C4=CC=CC=C24.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Adrenergic Receptor
In vitro	Maprotiline inhibits HERG channels expressed in HEK cells with an IC50 of 5.2 μM and HERG channels expressed in oocytes with an IC50 of 24 μM. Maprotiline blocks open channels but has no significant effect on closed channels. Maprotiline is atetracyclic antidepressant, which strongly inhibits the uptake of noradrenaline, though it is notable in its lack of inhibition of serotonergic uptake. Maprotiline also has markedly less pronounced alpha-adrenergic blocking activity than amitriptyline. Maprotiline decreases cell viability in a concentration- and time-dependent manner in Neuro-2a cells. Maprotiline induces apoptosis and increases caspase-3 activation. Maprotiline also induces [Ca(2+)](i) increases which involves the mobilization of intracellular Ca(2+) stored in the endoplasmic reticulum.
In vivo	Maprotiline results in significantly increases GluR1 and GluR2/3 subunit expression in the nucleus accumbens and dorsal striatum of mice as detected by immunohistochemistry; and significantly increases GluR1 and GluR2/3 expression in the hippocampus, as demonstrated by Western blot analysis. Maprotiline has a potent anti-inflammatory effect in rats and this effect is linked to the peripheral and supraspinal actions of the drug. Maprotiline impairs learning when administered before training, but no statistically significant effect is evident when administered after training.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16423345/ [2] https://pubmed.ncbi.nlm.nih.gov/16159672/ [3] https://pubmed.ncbi.nlm.nih.gov/23219590/ [4] https://pubmed.ncbi.nlm.nih.gov/19091461/ [5] https://pubmed.ncbi.nlm.nih.gov/20574769/ [6] https://pubmed.ncbi.nlm.nih.gov/10699652/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04200066	Withdrawn	Glioblastoma\|Brain Tumor	University of Rochester	June 1 2022	Phase 1

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Maprotiline HCl Adrenergic Receptor antagonist

Chemical Structure

Molecular Weight: 313.86