product name SB742457
Description: SB742457 (also known as GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, it exhibits >100-fold selectivity over other receptors. In addition, because of the orally bioavailable, SB742457 has been reported to promote brain penetration in rat over previously developed compounds. Besides, subchronic daily oral pre-dosing of SB742457 (1.5mg/kg) has been noted to significantly induce by the cholinergic antagonist scopolamine (0.5mg/kg) in a novel object recognition paradigm.
References: Neurotherapeutics. 2008 Jul;5(3):458-69.
353.44
Formula
C19H19N3O2S
CAS No.
607742-69-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 78 mg/mL (220.7 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (5.7 mM)
Solubility (In vivo)
2% DMSO, 48% PEG300, 2% Tween 80 and 48% water: 5mg/mL
Synonyms
GSK 742457
other peoduct :
| In Vitro |
In vitro activity: SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects. SB-742457 is a novel cognitive enhancing agent for Alzheimers disease. SB-742457 is a potential agent added to stablize donepezil treatment in subjects with mild-to-moderate Alzheimers disease. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | SB-742457 is a potent and selective 5-HT6 receptor antagonist that is shown to reverse a scopolamine induced learning deficit in the novel object recognition test and to enhance performance in a water maze task by aged rats. |
| Animal model | |
| Formulation & Dosage | |
| References | Neurotherapeutics. 2008 Jul;5(3):458-69. |
