Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Intepirdine HCl (GSK-742457; SB742457; RVT-101), the hydrochloride salt of Intepirdine, is a novel, potent and highly selective 5-HT6 receptor antagonist with pKi of 9.63; it exhibits >100-fold selectivity over other receptors. Potential benefits of intelepirdine include improved learning, memory, and cognitive function. Phase II clinical trials revealed some preliminary efficacy, and GlaxoSmithKline was studying it for the treatment of Alzheimer's disease. Age-related declines in delayed non-match-to-sample performance (DNMS) can be reversed by SB742457. SB742457 exhibits pro-cognitive effects that are increasingly evident in AD patients.
ln Vitro |
Intepirdine (SB742457), a 5-HT6 receptor antagonist, which is also present in Alzheimer disease (AD) patients, emphasizes the therapeutic potential of this mechanistic strategy. Devastating neurological conditions like depression and psychosis are common in Alzheimer's disease, which is marked by a progressive decline in cognitive function along with behavioral and psychological syndromes. Preclinical research in rodents and primates has cleared more light on the role of this receptor subtype, as has the subsequent development of selective 5-HT6 receptor antagonists. It is becoming more and more evident that blocking 5-HT6 receptors improves cognitive function across a broad range of learning and memory paradigms and also has anxiolytic and antidepressant-like effects. SB742457, or intepirdine, is generally well tolerated, safe, and possibly effective in treating Alzheimer's disease.
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References |
Molecular Formula |
C19H20CLN3O2S
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Molecular Weight |
389.9
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Exact Mass |
389.1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4.Cl
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InChi Key |
BWLWNUQEZNYKAU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H19N3O2S.ClH/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;1H
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Chemical Name |
3-(benzenesulfonyl)-8-piperazin-1-ylquinoline;hydrochloride
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Synonyms |
GSK-742457; SB-742457; RVT-101; Intepirdine HCl
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5648 mL | 12.8238 mL | 25.6476 mL | |
5 mM | 0.5130 mL | 2.5648 mL | 5.1295 mL | |
10 mM | 0.2565 mL | 1.2824 mL | 2.5648 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.
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.
(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.
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 |