SB-215505
Based on 1 Customer Validation
SB-215505 is an orally active and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.91%
- No. CAS: 162100-15-4
- Fòrmula: C19H16ClN3O
- Peso molecular:337.80
-
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
Ver todos los productos específicos de isoformas 5-HT Receptor
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
5-HT2B Receptor 8.3 (pKi) |
5-HT2A Receptor 6.77 (pKi) |
5-HT2C Receptor 7.66 (pKi) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
13 nM
Compound: SB-215505
|
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
|
[PMID: 19307114] |
| CHO-K1 | IC50 |
64 nM
Compound: SB-215505
|
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
|
[PMID: 19307114] |
In Vitro
SB-215505 is 30 fold selective for the 5-HT2B over the 5-HT2A receptor, and only marginally selective over the 5-HT2C receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Sprague-Dawley rats weighing 230-260 g[2]
-
Dosage:0.1, 0.3 and 1.0 mg/kg
-
Administration:IP; two doses (4 days between two doses)
-
Result:Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.
Chemical Information
-
No. CAS 162100-15-4
-
Appearance Solid
-
Peso molecular 337.80
-
Fòrmula C19H16ClN3O
-
Color Off-white to light brown
-
SMILES
O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=C4C=CC=NC4=CC=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
In Vitro:
DMSO : 25 mg/mL (74.01 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 (290 KB)
-
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. C Reavill, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4. [Content Brief]
[2]. Sandor Kantor, et al. Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. J Pharmacol. 2004 Aug;142(8):1332-42. [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 | 2.9603 mL | 14.8017 mL | 29.6033 mL | 74.0083 mL |
| 5 mM | 0.5921 mL | 2.9603 mL | 5.9207 mL | 14.8017 mL | |
| 10 mM | 0.2960 mL | 1.4802 mL | 2.9603 mL | 7.4008 mL | |
| 15 mM | 0.1974 mL | 0.9868 mL | 1.9736 mL | 4.9339 mL | |
| 20 mM | 0.1480 mL | 0.7401 mL | 1.4802 mL | 3.7004 mL | |
| 25 mM | 0.1184 mL | 0.5921 mL | 1.1841 mL | 2.9603 mL | |
| 30 mM | 0.0987 mL | 0.4934 mL | 0.9868 mL | 2.4669 mL | |
| 40 mM | 0.0740 mL | 0.3700 mL | 0.7401 mL | 1.8502 mL | |
| 50 mM | 0.0592 mL | 0.2960 mL | 0.5921 mL | 1.4802 mL | |
| 60 mM | 0.0493 mL | 0.2467 mL | 0.4934 mL | 1.2335 mL |
SB-215505 Related Classifications
HY-18596 Related Classifications
Powered by Bioz