| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
SB258585 targets the serotonin 5-HT6 receptor, a G protein-coupled receptor that is predominantly expressed in the central nervous system, particularly in regions involved in cognition and memory such as the hippocampus and cortex. By acting as a potent and selective antagonist at the 5-HT6 receptor with a Ki of 8.9 nM, SB258585 blocks 5-HT6 receptor-mediated signaling. This modulation of serotonergic signaling affects neurotransmitter release and synaptic plasticity, offering insights into serotonergic pathways. The compound shows >160-fold selectivity over other 5-HT receptor subtypes.
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| ln Vitro |
In vitro, SB258585 acts as a high-affinity ligand for the 5-HT6 receptor. It binds with high affinity to a single receptor population in human recombinant 5-HT6 receptor cell lines and native 5-HT6 receptors. The compound has a Ki of 8.9 nM and shows >160-fold selectivity over other 5-HT receptor subtypes. Its potent and selective binding to 5-HT6 receptors makes it a valuable tool for studying the role of 5-HT6 receptors in cognitive function and neuropsychiatric disorders.
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| ln Vivo |
In vivo, SB258585 has been used in neuroscience research to study cognitive function, memory, and neuropsychiatric disorders such as Alzheimer's disease, schizophrenia, and depression. By blocking 5-HT6 receptor activity, the compound modulates neurotransmitter release and synaptic plasticity. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. The compound is primarily a research tool for studying serotonergic signaling pathways.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SB258585 are radioligand binding assays using membrane preparations from cells expressing recombinant human 5-HT6 receptors or native receptors from brain tissue. The compound's binding affinity (Ki) is determined by its ability to displace a labeled 5-HT6 receptor ligand such as [3H]LSD or [3H]5-HT. Selectivity is confirmed by testing the compound's binding affinity for other 5-HT receptor subtypes. These assays provide quantitative measures of the compound's potency and selectivity.
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| Cell Assay |
In vitro cellular assays for SB258585 are performed using cell lines expressing recombinant human 5-HT6 receptors, such as HEK293 or CHO cells. Cells are treated with SB258585, and 5-HT6 receptor-mediated signaling is assessed by measuring cAMP accumulation (since 5-HT6 receptors are Gs-coupled and stimulate adenylyl cyclase). The compound's ability to inhibit agonist-stimulated cAMP production is measured. These assays confirm the functional antagonism of SB258585 at 5-HT6 receptors.
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| Animal Protocol |
In vivo animal experiments for SB258585 are conducted in rodent models to study cognitive function and neuropsychiatric disorders. Mice or rats are administered SB258585 via oral or intraperitoneal injection, and cognitive performance is assessed using behavioral tests such as the Morris water maze, novel object recognition, or passive avoidance tests. The compound's effects on neurotransmitter release in the brain can be assessed using microdialysis. These studies evaluate the compound's ability to modulate 5-HT6 receptor-mediated effects on cognition and behavior.
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| ADME/Pharmacokinetics |
SB258585 Hydrochloride has a molecular weight of 523.82 g/mol and a molecular formula of C18H22IN3O3S·HCl. The compound is soluble in DMSO and other organic solvents. It is stable at -20°C for long-term storage. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As an orally active compound, SB258585 is expected to have favorable pharmacokinetic properties for central nervous system applications.
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| Toxicity/Toxicokinetics |
SB258585 Hydrochloride has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. No significant toxicity has been reported in the available literature. As a selective 5-HT6 receptor antagonist, SB258585 may have a favorable safety profile with reduced risk of off-target effects. However, comprehensive toxicology studies would be necessary to fully assess the compound's safety for clinical development.
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| References | |
| Additional Infomation |
SB258585 Hydrochloride is a potent, selective, and orally active 5-HT6 receptor antagonist with a Ki of 8.9 nM and >160-fold selectivity over other 5-HT receptor subtypes. It is used in neuroscience research to study cognitive function, memory, and neuropsychiatric disorders such as Alzheimer's disease, schizophrenia, and depression. By blocking 5-HT6 receptor activity, the compound modulates neurotransmitter release and synaptic plasticity. SB258585 is a research compound and is not an approved drug.
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| Molecular Formula |
C18H23CLIN3O3S
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|---|---|
| Molecular Weight |
523.815994501114
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| Exact Mass |
523.019
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| CAS # |
1216468-02-8
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| Related CAS # |
209480-63-7;1216468-02-8 (HCl);
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| PubChem CID |
53429667
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| Appearance |
Off-white to light brown solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
540
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(CC1)C2=C(C=CC(=C2)NS(=O)(=O)C3=CC=C(C=C3)I)OC.Cl
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| InChi Key |
BFGOZFXMAJBFGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22IN3O3S.ClH/c1-21-9-11-22(12-10-21)17-13-15(5-8-18(17)25-2)20-26(23,24)16-6-3-14(19)4-7-16;/h3-8,13,20H,9-12H2,1-2H3;1H
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| Chemical Name |
4-iodo-N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]benzenesulfonamide;hydrochloride
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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) |
DMSO : ~125 mg/mL (~238.63 mM)
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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 | 1.9091 mL | 9.5453 mL | 19.0905 mL | |
| 5 mM | 0.3818 mL | 1.9091 mL | 3.8181 mL | |
| 10 mM | 0.1909 mL | 0.9545 mL | 1.9091 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.
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