Benztropine mesylate

Synonyms: Cogentin mesylate, Benztropine methanesulfonate

Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.

Benztropine mesylate Chemical Structure

Benztropine mesylate Chemical Structure

CAS No. 132-17-2

Purity & Quality Control

Benztropine mesylate Related Products

Biological Activity

Description Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Targets
DAT [1]
118 nM
In vitro
In vitro

Benztropine inhibits MTSET-induced inhibition of [3H]WIN binding to Wild-type dopamine transporter with EC50 of 28 μM in concentration-dependent manner. Benztropine has a protective ratio (EC50/inhibiting [3H]WIN (4 nm) binding with IC50) of 32 in X-A342C DAT construct by protecting Cys-342 from reaction. [2] The apparent equilibrium dissociation constant of W84L DAT for benztropine is significantly higher than that of WT in the absence of sodium but this difference becomes smaller in the presence of 130 mM sodium in HEK-293 cells incubated with [3H]CFT. The apparent equilibrium dissociation constant of D313N DAT for benztropine displays a modest increase in the presence of 130 mM sodium in HEK-293 cells incubated with [3H]CFT. The apparent equilibrium dissociation constant value for benztropine at the double mutant (W84L D313N DAT) is in general close to that at one of the single mutants. [3]

In Vivo
In vivo

Benztropine (3.0 mg/day) is effective in improving tremor and the motor score of the United Parkinson's Disease Rating Scale without adverse events like leukopenia. [4] Benztropine (5 mg/kg and 25 mg/kg) shows dose-dependent elevations in extracellular dopamine in the striatum of the rat. [5]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00715377 Terminated
Schizophrenia|Schizoaffective Disorder|Schizophreniform Disorder|Delusional Disorder|Psychotic Disorders
Centre for Addiction and Mental Health
June 2007 Not Applicable

Chemical Information & Solubility

Molecular Weight 403.53 Formula

C21H25NO.CH4SO3

CAS No. 132-17-2 SDF Download Benztropine mesylate SDF
Smiles CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4.CS(=O)(=O)O
Storage (From the date of receipt)

In vitro
Batch:

Water : 81 mg/mL

Ethanol : 81 mg/mL

DMSO : 50 mg/mL ( (123.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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 %

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Benztropine mesylate | Benztropine mesylate supplier | purchase Benztropine mesylate | Benztropine mesylate cost | Benztropine mesylate manufacturer | order Benztropine mesylate | Benztropine mesylate distributor