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

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

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

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 77 In-stock
Solid
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Based on 2 publication(s) in Google Scholar

Intepirdine Related Antibodies

Top Publications Citing Use of Products

View All 5-HT Receptor Isoform Specific Products:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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)

Cellular Effect
Cell Line Type Value Description References
Astrocyte CC50
> 1 μM
Compound: Intepirdine
Toxicity in mouse C8-D1A astrocytes assessed as reduction in cell viability by MTT assay
Toxicity in mouse C8-D1A astrocytes assessed as reduction in cell viability by MTT assay
[PMID: 33439019]
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.

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

Intepirdine Related Antibodies
Clinical Trial
Molecular Weight

353.44

Formula

C19H19N3O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (141.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8293 mL 14.1467 mL 28.2933 mL 70.7334 mL
5 mM 0.5659 mL 2.8293 mL 5.6587 mL 14.1467 mL
10 mM 0.2829 mL 1.4147 mL 2.8293 mL 7.0733 mL
15 mM 0.1886 mL 0.9431 mL 1.8862 mL 4.7156 mL
20 mM 0.1415 mL 0.7073 mL 1.4147 mL 3.5367 mL
25 mM 0.1132 mL 0.5659 mL 1.1317 mL 2.8293 mL
30 mM 0.0943 mL 0.4716 mL 0.9431 mL 2.3578 mL
40 mM 0.0707 mL 0.3537 mL 0.7073 mL 1.7683 mL
50 mM 0.0566 mL 0.2829 mL 0.5659 mL 1.4147 mL
60 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1789 mL
80 mM 0.0354 mL 0.1768 mL 0.3537 mL 0.8842 mL
100 mM 0.0283 mL 0.1415 mL 0.2829 mL 0.7073 mL
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Intepirdine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Intepirdine607742-69-8SB-742457 GSK-742457 RVT-101SB742457SB 742457GSK742457GSK 742457GSK-742457RVT101RVT 101RVT-1015-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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