Bemesetron
Based on 1 Customer Validation
Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Neuroprotective effect.
For research use only. We do not sell to patients.
- Purity: 99.05%
- CAS No.: 40796-97-2
- Formula: C15H17Cl2NO2
- Molecular Weight:314.21
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT3 Receptor 0.33 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
6.9 x 10-9 M
Compound: MDL 72222
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Displacement of [3H]BRL 43694 from human recombinant 5HT3 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
Displacement of [3H]BRL 43694 from human recombinant 5HT3 receptor expressed in CHO cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
| HEK293 | IC50 |
0.011 μM
Compound: MDl 72222
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Displacement of [3H]GR65630 from human recombinant 5HT3 receptor expressed in HEK293 cells after 60 mins
Displacement of [3H]GR65630 from human recombinant 5HT3 receptor expressed in HEK293 cells after 60 mins
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[PMID: 23403082] |
Blockade of 5-HT3 receptor with Bemesetron (MDL7222) reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Bemesetron (0.01, 0.1 and 1 μM, 15 hours) and Y25130 (0.05, 0.5 and 5 μM) concentration-dependently reduce the H2O2-induced decrease of MTT reduction showing 74.9±2.4 and 79.0 ±2.5% with 1 μM and 5 μM, respectively, which are maximal effects[2].
Pretreatment (20 minutes) with Bemesetron (1 μM), Y25130 (5 μM) or MK-801 (10 μM) significantly, but not completely, inhibits the H2O2-induced elevation of [Ca2+]c[2].
Bemesetron (1 μM, 15 hours) significantly blocks the H2O2-induced increase of caspase-3 immunoreactivity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary cortical neuronal cells
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Concentration:0.01-1 μM
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Incubation Time:20 minutes (pretreatment); 15 hours (post-incubation)
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Result:Concentration-dependently reduced the H2O2-induced decrease of MTT reduction showing 74.9±2.4% with 1 μM, which was maximal effect.
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Cell Line:Primary cortical neuronal cells
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Concentration:1 μM
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Incubation Time:15 hours
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Result:Blocked significantly the H2O2-induced increase of caspase-3 immunoreactivity.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male adult albino mice, weighing 26-36 g[3]
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Dosage:0.1-10 mg/kg
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Administration:Intraperitoneally injected, 20 min (pretreatment) +180 min (treatment)
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Result:Reduced catalepsy significantly at a dose of 1 mg/kg, whilst 10 mg/kg potentiated the phenomenon and 0.1 mg/kg was found to be without effect.
Chemical Information
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CAS No. 40796-97-2
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Appearance Solid
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Molecular Weight 314.21
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Formula C15H17Cl2NO2
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Color White to off-white
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SMILES
O=C(O[C@@H]1C[C@@H](N2C)CC[C@@H]2C1)C3=CC(Cl)=CC(Cl)=C3
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Synonyms
MDL 72222
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 2 mg/mL (6.37 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Peters JA, et al. An electrophysiological investigation of the properties of 5-HT3 receptors of rabbit nodose ganglion neurones in culture. Br J Pharmacol. 1993 Oct;110(2):665-76. [Content Brief]
[2]. Lee HJ, et al. Blockade of 5-HT(3) receptor with MDL7222 and Y25130 reduces hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Life Sci. 2005 Dec 5;78(3):294-300. [Content Brief]
[3]. Silva SR, et al. Effects of 5-HT3 receptor antagonists on neuroleptic-induced catalepsy in mice. Neuropharmacology. 1995 Jan;34(1):97-9. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1826 mL | 15.9129 mL | 31.8258 mL | 79.5646 mL |
| 5 mM | 0.6365 mL | 3.1826 mL | 6.3652 mL | 15.9129 mL |
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