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Benztropine mesylate Dopamine Receptor inhibitor

Name: Benztropine mesylate
Brand: Selleck Chemicals
SKU: S3163
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S3163

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

Chemical Structure

Molecular Weight: 403.53

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.94%

99.94

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Chemical Information, Storage & Stability

Molecular Weight	403.53	Formula	C₂₁H₂₅NO.CH₄SO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	132-17-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Cogentin mesylate, Benztropine methanesulfonate			Smiles	CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4.CS(=O)(=O)O

Solubility

In vitro
Batch:

Water : 81 mg/mL

Ethanol : 81 mg/mL

DMSO : 50 mg/mL (123.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.5mg/ml (6.20mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.35mg/ml (0.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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

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.

Mechanism of Action

Targets/IC₅₀/Ki	DAT ^[1] 118 nM
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	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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15857139/ [2] https://pubmed.ncbi.nlm.nih.gov/11395483/ [3] https://pubmed.ncbi.nlm.nih.gov/15140185/ [4] https://pubmed.ncbi.nlm.nih.gov/9109903/ [5] https://pubmed.ncbi.nlm.nih.gov/3666010/

Clinical Trial Information

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

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

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