SB228357
Based on 1 Customer Validation
SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.43%
- No. CAS: 181629-93-6
- Fòrmula: C22H17F4N3O2
- Peso molecular:431.38
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Neuronal Signaling Compound Library
HY-L013
-
Orally Active Compound Library
HY-L061
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Anti-Parkinson's Disease Compound Library
HY-L085
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Antidepressant Compound Library
HY-L108
-
5-HT Receptor Compound Library
HY-L121
-
Coagulation and Anti-coagulation Compound Library
HY-L136
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Lactylation Compound Library
HY-L249
Ver todos los productos específicos de isoformas 5-HT Receptor
More
Actividad biológica
|
5-HT2A Receptor |
5-HT2B Receptor |
5-HT2C Receptor |
5-HT2A Receptor 6.9 (pKi) |
5-HT2C Receptor 9 (pKi) |
5-HT2B Receptor 8 (pKi) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.01 μM
Compound: 2
|
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay
|
[PMID: 24900481] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Sprague Dawley rats (200-250 g) injected with Haloperidol[2]
-
Dosage:0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg
-
Administration:Oral administration; for 90 minutes
-
Result:Significantly reversed Haloperidol-induced catalepsy.
Chemical Information
-
No. CAS 181629-93-6
-
Appearance Solid
-
Peso molecular 431.38
-
Fòrmula C22H17F4N3O2
-
Color White to off-white
-
SMILES
O=C(N1CCC2=C1C=C(C(F)(F)F)C(OC)=C2)NC3=CC(C4=CC=CN=C4)=CC(F)=C3
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 125 mg/mL (289.77 mM; ultrasonic and warming and heat to 60°C; 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Bromidge SM, et al. Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem. 2000 Mar 23;43(6):1123-34. [Content Brief]
[2]. Reavill C, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3181 mL | 11.5907 mL | 23.1814 mL | 57.9535 mL |
| 5 mM | 0.4636 mL | 2.3181 mL | 4.6363 mL | 11.5907 mL | |
| 10 mM | 0.2318 mL | 1.1591 mL | 2.3181 mL | 5.7954 mL | |
| 15 mM | 0.1545 mL | 0.7727 mL | 1.5454 mL | 3.8636 mL | |
| 20 mM | 0.1159 mL | 0.5795 mL | 1.1591 mL | 2.8977 mL | |
| 25 mM | 0.0927 mL | 0.4636 mL | 0.9273 mL | 2.3181 mL | |
| 30 mM | 0.0773 mL | 0.3864 mL | 0.7727 mL | 1.9318 mL | |
| 40 mM | 0.0580 mL | 0.2898 mL | 0.5795 mL | 1.4488 mL | |
| 50 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 1.1591 mL | |
| 60 mM | 0.0386 mL | 0.1932 mL | 0.3864 mL | 0.9659 mL | |
| 80 mM | 0.0290 mL | 0.1449 mL | 0.2898 mL | 0.7244 mL | |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2318 mL | 0.5795 mL |
SB228357 Related Classifications
HY-103154 Related Classifications
Powered by Bioz