| Size | Price | Stock | Qty |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Benztropine mesylate (NSC-42199; ST-50997629; NSC 42199; ST 50997629; Cogentin; MLS000737056), the mesilate salt of Benztropine, is a highly potent dopamine transporter (DAT) inhibitor used for the treatment of symptoms of Parkinson's disease such as involuntary tremor and dystonia. It suppresses the dopamine transporter with an IC50 of 118 nM. Benztropine is a synthetic substance that acts centrally to sabotage M1 muscarinic acetylcholine receptors. It is derived from the combination of atropine and diphenhydramine.
| Targets |
Human D2 Receptor
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| ln Vitro |
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| ln Vivo |
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| Cell Assay |
Cell Line: MDA-MB-231 cells
Concentration: 0.1 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM Incubation Time: 72 hours Result: Inhibited the cell growth of MDA-MB-231 cells with an IC50 of ~5 μM. |
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| Animal Protocol |
Balb/c mice bearing 4T1 breast tumors
1.5 mg/kg Injection; 3 weeks |
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| References | ||
| Additional Infomation |
Benzatropine is tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments. It has a role as an antiparkinson drug, a parasympatholytic, an antidyskinesia agent, a muscarinic antagonist and a oneirogen.
Benztropine is an Anticholinergic and Antihistamine. The mechanism of action of benztropine is as a Cholinergic Antagonist and Histamine Receptor Antagonist. A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine. See also: Benztropine (annotation moved to); Benztropine Mesylate (annotation moved to). |
| Molecular Formula |
C22H29NO4S
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|---|---|---|
| Molecular Weight |
403.53
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| Exact Mass |
403.181
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| Elemental Analysis |
C, 65.81; H, 6.78; N, 3.49; O, 15.94; S, 7.99
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| CAS # |
132-17-2
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| Related CAS # |
Benztropine; 86-13-5; Benztropine-13C,d3 mesylate; Benztropine-d3 mesylate; 202529-16-6
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| PubChem CID |
1201549
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| Appearance |
White to light yellow crystalline powder
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| Boiling Point |
547.8ºC at 760 mmHg
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| Melting Point |
135 °C(lit.)
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| Flash Point |
285.1ºC
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| Vapour Pressure |
7.83E-13mmHg at 25°C
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| LogP |
4.94
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
340
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S(C([H])([H])[H])(=O)(=O)O[H].O(C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H])C1([H])C([H])([H])[C@]2([H])C([H])([H])C([H])([H])[C@]([H])(C1([H])[H])N2C([H])([H])[H]
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| InChi Key |
CPFJLLXFNPCTDW-IIPFOPBBSA-N
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| InChi Code |
InChI=1S/C21H25NO.CH4O3S/c1-22-18-12-13-19(22)15-20(14-18)23-21(16-8-4-2-5-9-16)17-10-6-3-7-11-17;1-5(2,3)4/h2-11,18-21H,12-15H2,1H3;1H3,(H,2,3,4)/t18-,19+,20?;
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| Chemical Name |
(1R,5S)-3-benzhydryloxy-8-methyl-8-azabicyclo[3.2.1]octane;methanesulfonic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 100 mg/mL (247.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4781 mL | 12.3907 mL | 24.7813 mL | |
| 5 mM | 0.4956 mL | 2.4781 mL | 4.9563 mL | |
| 10 mM | 0.2478 mL | 1.2391 mL | 2.4781 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00000333 | Completed | Drug: Benztropine | Cocaine-Related Disorders | National Institute on Drug Abuse (NIDA) |
May 2001 | Phase 2 |
| NCT00000793 | Completed | Drug: Benztropine mesylate Drug: Mexiletine hydrochloride |
HIV Infections Peripheral Nervous System Disease |
National Institute of Allergy and Infectious Diseases (NIAID) |
October 1997 | Phase 2 |
| NCT00018200 | Completed | Drug: Benztropine Drug: Fluoxetine |
Back Pain Sciatica |
US Department of Veterans Affairs | April 1999 | Phase 2 |
| NCT00066937 | Completed | Behavioral: Disease MGT Behavioral: CBT |
Temporomandibular Joint Disorders |
Johns Hopkins University | November 2002 | Phase 2 |
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