1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Intepirdine

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

Cat. No.: HY-14339 Purity: 98.92%
Handling Instructions

Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.

For research use only. We do not sell to patients.

Intepirdine Chemical Structure

Intepirdine Chemical Structure

CAS No. : 607742-69-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 410 In-stock
Estimated Time of Arrival: December 31
50 mg USD 690 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.

IC50 & Target

5-HT6 Receptor

9.63 (pKi)

In Vitro

Intepirdine (SB742457), a 5-HT6 receptor antagonist, which extends into Alzheimer disease (AD) sufferers further highlights the therapeutic promise of this mechanistic approach. Alzheimer's disease is a devastating neurological condition characterized by a progressive decline in cognitive performance accompanied by behavioral and psychological syndromes, such as depression and psychosis. With the subsequent development of selective 5-HT6 receptor antagonists, preclinical studies in rodents and primates have elucidated the function of this receptor subtype in more detail. It is increasingly clear that blockade of 5-HT6 receptors leads to an improvement of cognitive performance in a wide variety of learning and memory paradigms and also results in anxiolytic and antidepressant-like activity. Intepirdine (SB742457) is generally safe and well tolerated and may be efficacious in Alzheimer disease.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

353.44

Formula

C₁₉H₁₉N₃O₂S

CAS No.

607742-69-8

SMILES

O=S(C1=CC=CC=C1)(C2=CC(C=CC=C3N4CCNCC4)=C3N=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (141.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8293 mL 14.1467 mL 28.2933 mL
5 mM 0.5659 mL 2.8293 mL 5.6587 mL
10 mM 0.2829 mL 1.4147 mL 2.8293 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

IntepirdineSB-742457 GSK-742457 RVT-101SB742457SB 742457GSK742457GSK 742457GSK-742457RVT101RVT 101RVT-1015-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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Product Name:
Intepirdine
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HY-14339
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