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      Intepirdine (SB-742457; GSK-742457; RVT-101)
      Intepirdine (SB-742457; GSK-742457; RVT-101)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1020
      CAS #: 607742-69-8Purity ≥98%

      Description: Intepirdine (formerly GSK-742457; RVT-101; SB742457; SB 742457; GSK742457; SB-742457; RVT 101) is a potent and highly selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects. It inhibits 5-HT6 with a pKi of 9.63, and exhibits >100-fold selectivity for 5-HT6 over other receptors.  

      References: Neurotherapeutics. 2008 Jul;5(3):458-69. 

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      Molecular Weight (MW)353.44
      FormulaC19H19N3O2S 
      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
      SynonymsGSK 742457; GSK-742457; RVT-101; SB742457; SB 742457; GSK742457; SB-742457; RVT 101; RVT101


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      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 Alzheimer's disease. SB-742457 is a potential agent added to stablize donepezil treatment in subjects with mild-to-moderate Alzheimer's disease.

      In VivoSB-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 modelN/A
      Formulation & DosageN/A
      References

      Neurotherapeutics. 2008 Jul;5(3):458-69.  

      These protocols are for reference only. InvivoChem does not independently validate these methods.

       
      SB742457
      Effects of the 5-HT2A receptor agonist TCB-2 and the 5-HT7 receptor agonist AS 19 on smooth muscle cell membrane potential in endothelium-intact preparations. Br J Pharmacol. 2011 Oct; 164(3): 979–991.
      		 
      SB742457
      Effects of SB269970, glibenclamide and Rp-cAMPS on 5-HT-induced changes in smooth muscle cell membrane potential in endothelium-intact preparations. Br J Pharmacol. 2011 Oct; 164(3): 979–991.
      		 
      SB742457
      Effects of SB269970 with or without sarpogrelate on 5-HT-induced changes in smooth muscle cell membrane potential in endothelium-denuded preparations. Br J Pharmacol. 2011 Oct; 164(3): 979–991.

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