Benztropine mesylate
Based on 5 publication(s) in Google Scholar
Benztropine mesylate (Benzatropine mesylate) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
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- Pureté : 99.85%
- CAS No.: 132-17-2
- Formule: C22H29NO4S
- Masse moléculaire:403.54
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Benztropine mesylate
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Activité biologique
Description
IC50 & Target
[1]|
Human D2 Receptor |
In Vitro
Benztropine mesylate (0.1-10 μM; 72 hours) treatment inhibits the cell growth of MDA-MB-231 cells with an IC50 of ~5 μM. In MDA-MB-231 cells and 4T1-luc2 cells, Benztropine mesylate reduces the size as well as the number of mammospheres significantly in a dose-dependent manne[1].
Benztropine mesylate inhibits functions of cancer stem cells (CSCs) via the acetylcholine receptors, dopamine transporters/receptors, and/or histamine receptors[1].
Benztropine mesylate induces the differentiation of oligodendrocytes through M1 and M3 muscarinic receptors and enhanced re-myelination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.1 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:72 hours
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Result:Inhibited the cell growth of MDA-MB-231 cells with an IC50 of ~5 μM.
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Cell Line:MDA-MB-231 cells
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Concentration:0, 1, 2, 5 μM
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Incubation Time:4-6 days
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Result:Suppressed mammosphere formation and self-renewal capacities of BCSCs in a dose-dependent manner in vitro.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice bearing 4T1 breast tumors
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Dosage:1.5 mg/kg
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Administration:Injection; 3 weeks
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Result:Reduced the tumor size and weight significantly without body weight changing.
Chemical Information
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CAS No. 132-17-2
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Appearance Solid
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Masse moléculaire 403.54
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Formule C22H29NO4S
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Color White to off-white
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SMILES
CN1[C@H]2CC(OC(C3=CC=CC=C3)C4=CC=CC=C4)C[C@@H]1CC2.CS(=O)(O)=O
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Synonyms
Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
2024 Aug;632(8025):686-694. PMID: 39112701 -
J Clin Invest
2022 Feb 15;132(4):e150101. PMID: 34964720 -
Front Cell Neurosci
Differential Regulation of Adhesion and Phagocytosis of Resting and Activated Microglia by Dopamine. [Abstract]2018 Sep 11:12:309. PMID: 30254570
Benztropine mesylate purchased from MedChemExpress. Usage Cited in: Front Cell Neurosci. 2018 Sep 11:12:309. [Abstract]
p38MAPK activation by dopamine (DA) can be inhibited by selective DAT blockers (Benztropine and Vanoxerine; 2 μM each) and PMAT blocker (Decynium; 2 μM). Combination of DAT and PMAT blockers further inhibits the activation of p38MAPK.
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Viruses
Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]2021 Jun 28;13(7):1255. PMID: 34203149 -
PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351
Solvant et solubilité
In Vitro:
H2O : 100 mg/mL (247.81 mM; Need ultrasonic)
DMSO : 100 mg/mL (247.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (247.81 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Jihong Cui, et al. New use of an old drug: inhibition of breast cancer stem cells by benztropine mesylate. Oncotarget. 2017 Jan 3;8(1):1007-1022. [Content Brief]
[2]. Santosh S Kulkarni, et al. Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors. Bioorg Med Chem. 2006 Jun 1;14(11):3625-34. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.4781 mL | 12.3903 mL | 24.7807 mL | 61.9517 mL |
| 5 mM | 0.4956 mL | 2.4781 mL | 4.9561 mL | 12.3903 mL | |
| 10 mM | 0.2478 mL | 1.2390 mL | 2.4781 mL | 6.1952 mL | |
| 15 mM | 0.1652 mL | 0.8260 mL | 1.6520 mL | 4.1301 mL | |
| 20 mM | 0.1239 mL | 0.6195 mL | 1.2390 mL | 3.0976 mL | |
| 25 mM | 0.0991 mL | 0.4956 mL | 0.9912 mL | 2.4781 mL | |
| 30 mM | 0.0826 mL | 0.4130 mL | 0.8260 mL | 2.0651 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6195 mL | 1.5488 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4956 mL | 1.2390 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4130 mL | 1.0325 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7744 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6195 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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