Antibodies
Benztropine mesylate
- 貨號 Cat. No.
- S3163
- 規格 Size
- 10mM/1mLã€50mg
- 品牌 Brand
- Selleckchem
Description
Benztropine mesylate
Catalog No.S3163
Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
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Biological Activity
| Description | Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM. | |||||
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| Targets | DAT | |||||
| IC50 | 118 nM [1] | |||||
| 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] | |||||
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Protocol(Only for Reference)
Kinase Assay: [1]
| Binding assay | Rats are decapitated and their brains are quickly removed and placed in ice-cold 0.32 M sucrose. The striatal tissue is removed and homogenized in 20 volumes of 0.32 M sucrose using a Polytron homogenizer. The supernatant obtained after centrifugation for 10 min at 0°C (S1 fraction) is removed and centrifuged for 20 min at 2×104 g and 0℃ to obtain the P2 fraction, which is then resuspended in 50 volumes (original wet weight) of ice-cold 25 mM sodium phosphate buffer (pH 7.7). Samples containing phosphate buffer, P2 suspension, Benztropine, water or cocaine 50 μM (to define non-specific binding) and [3H]WIN 2 nM are incubated for 2h at 0°C. |
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References
Chemical Information
Download Benztropine mesylate SDF
| Molecular Weight (MW) | 403.53 |
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| Formula | C21H25NO.CH4SO3 |
| CAS No. | 132-17-2 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 50 mg/mL (123 mM) |
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| Water | 81 mg/mL (200 mM) | ||
| Ethanol | 81 mg/mL (200 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 8-Azabicyclo[3.2.1]octane, 3-(diphenylmethoxy)-8-methyl-, (3-endo)-, methanesulfonate (1:1) |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.40353 | 4.0353 | 8.0706 | 12.1059 |
