209481-24-3
SB 271046 (Hydrochloride)
CAS: 209481-24-3
Molecular Formula: C20H22ClN3O3S2.HCl
209481-24-3 - Names and Identifiers
209481-24-3 - Physico-chemical Properties
| Molecular Formula | C20H22ClN3O3S2.HCl |
| Molar Mass | 488.45092 |
| Solubility | 10 mM in DMSO |
| Appearance | powder |
| Storage Condition | 2-8°C |
| In vitro study | SB-271046 acts on rat and pig striatum and human caudate shell membrane, effectively replacing [In the functional adenylate cyclase assay, SB-271046 is a competitive antagonist with a pA 2 of 8.7, this is in good agreement with its binding affinity. SB-271046 has no significant inhibitory activity against most human P450 enzymes. |
| In vivo study | In the maximum electroconvulsive seizure threshold (MEST) test in rats, SB-271046 in a wide range of doses, increasing the seizure threshold, the lowest effective oral dose is 0.1 mg/kg, and after 4 hours, the maximum effect is achieved. The level of anticonvulsant activity correlated well with SB-271046 blood concentrations (EC50 of 0.16 μm) and brain concentrations at 0.01 μm to 0.04 μm of C max. SB-271046-treated rats, a moderate cerebral penetrant (10%), with low blood clearance (7.7 mL/min/kg), good half-life (4.8 H), excellent oral bioavailability (>80%). SB-271046 treatment of the rat frontal cortex and dorsal hippocampus increased extracellular glutamate levels 3-fold and 2-fold, respectively, indicating that it can be used to treat cognitive and memory dysfunction. SB-271046 Wistar rats were fed orally at a dose of 20 mg/kg for 30 minutes and then trained. After 6 hours of training, it was found that Scopolamine(0.8 mg/kg, I. P.) treatment-induced amnesia. SB-271046 subcutaneous injection at a dose of 10 mg/kg) treatment of the frontal cortex of rats significantly increased the extracellular levels of glutamate and aspartate, which was Tetrodotoxin-dependent and reached a maximum, 375.4% and 215.3%, respectively, before injection. |
209481-24-3 - Risk and Safety
| WGK Germany | nwg |
209481-24-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.047 ml | 10.236 ml | 20.473 ml |
| 5 mM | 0.409 ml | 2.047 ml | 4.095 ml |
| 10 mM | 0.205 ml | 1.024 ml | 2.047 ml |
| 5 mM | 0.041 ml | 0.205 ml | 0.409 ml |
Last Update：2024-01-02 23:10:35
209481-24-3 - Reference Information
| biological activity | SB271046 is an orally bioavailable, selective 5-HT6 receptor antagonist with a pKi of 8.9, it is 200-fold more selective than acting on other 5-HT receptor subtypes. |
| Target | Value |
| 5-HT6 (Cell-free assay) | 8.92(pKi) |
Last Update：2024-04-10 22:29:15
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Product Name: SB 271046 (Hydrochloride) Visit Supplier Webpage Request for quotation
CAS: 209481-24-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 209481-24-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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