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

Alias: GSK 742457; GSK-742457; RVT-101; SB742457; SB 742457; GSK742457; SB-742457; RVT 101; RVT101

Cat No.:V1020 Purity: ≥98%

COA Product Data Instructions for use SDS

Intepirdine (SB-742457; GSK-742457; RVT-101) Chemical Structure CAS No.: 607742-69-8
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

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10mg
25mg
50mg
100mg
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1g
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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product 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 shows >100-fold selectivity for 5-HT6 over other receptors and inhibits 5-HT6 with a pKi of 9.63.

Biological Activity I Assay Protocols (From Reference)

Targets

5-HT₆ Receptor ( pKi = 9.63 )

ln Vitro

In vitro activity: SB-742457 is a selective antagonist of the 5-HT6 receptor that improves learning, memory, and cognitive function.[2] SB-742457 is a new Alzheimer's disease cognitive enhancer. Potential medication SB-742457 is added to subjects with mild-to-moderate Alzheimer's disease in order to stabilize their donepezil treatment.[1]

ln Vivo

SB-742457 is a potent and selective 5-HT6 receptor antagonist that has been demonstrated to improve elderly rats' performance in a water maze task and to reverse a learning deficit caused by scopolamine in the novel object recognition test.[1]

Animal Protocol

N/A

References

[1] Alzheimers Dement, 2006, 2, S631–S632 (abstract).

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

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

Physicochemical Properties

Molecular Formula

C19H19N3O2S

Molecular Weight

353.44

Exact Mass

353.12

Elemental Analysis

C, 64.57; H, 5.42; N, 11.89; O, 9.05; S, 9.07

CAS #

607742-69-8

Related CAS #

607742-69-8

Appearance

Solid powder

SMILES

C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4

InChi Key

JJZFWROHYSMCMU-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H19N3O2S/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22/h1-8,13-14,20H,9-12H2

Chemical Name

3-(benzenesulfonyl)-8-piperazin-1-ylquinoline

Synonyms

GSK 742457; GSK-742457; RVT-101; SB742457; SB 742457; GSK742457; SB-742457; RVT 101; RVT101

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 50~78 mg/mL (141.5~220.7 mM)

Water: <1 mg/mL

Ethanol: ~2 mg/mL (~5.7 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 2% DMSO , 48% PEG300, 2% Tween 80 and 48% water: 5mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02669433	Completed	Drug: RVT-101 35 mg Drug: RVT-101 70 mg	Dementia With Lewy Bodies	Axovant Sciences Ltd.	January 2016	Phase 2
NCT02585934	Completed	Drug: RVT-101 Drug: Placebo	Alzheimer's Disease	Axovant Sciences Ltd.	October 2015	Phase 3
NCT00710684	Completed	Drug: SB-742457 15mg Drug: SB-742457 35mg	Alzheimer's Disease	GlaxoSmithKline	July 1, 2008	Phase 2
NCT00708552	Completed	Drug: SB-742457 Drug: Placebo Drug: Donepezil	Alzheimer's Disease	GlaxoSmithKline	July 4, 2008	Phase 2
NCT00551772	Completed	Drug: SB-742457	Alzheimer's Disease	GlaxoSmithKline	August 2007	Phase 1

Biological Data

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.

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.
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.