| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
5-HT6 Receptor 9.02 (pKi) Human 5-HT6 Receptor 9.11 (pKi)
SB399885 targets the serotonin 5-HT6 receptor. It is a potent, competitive antagonist with high affinity for human recombinant (pKi 9.11; Ki 0.78 nM) and native human (pKi 9.02) 5-HT6 receptors. It shows >200-fold selectivity for 5-HT6 over other 5-HT receptors. By blocking 5-HT6 receptors, the compound modulates serotonergic signaling pathways involved in cognition, memory, and learning. |
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| ln Vitro |
In vitro, SB399885 acts as a potent and selective 5-HT6 receptor antagonist. Its activity is typically assessed by measuring its ability to inhibit 5-HT-stimulated cAMP accumulation in cells expressing 5-HT6 receptors. The compound shows pKi values of 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. It displays >200-fold selectivity for 5-HT6 over other 5-HT receptors. Standard in vitro assays include receptor binding studies using radiolabeled ligands such as [3H]-LSD and functional assays measuring cAMP accumulation.
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| ln Vivo |
In vivo, SB399885 displays cognitive enhancing properties in aged rat water maze and novel object recognition models. As a brain-penetrant and orally active 5-HT6 receptor antagonist, it is suitable for systemic administration in animal models. The compound has been studied for its potential in cognitive enhancement and treatment of cognitive disorders. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool to study 5-HT6 receptor function and cognitive processes.
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| Enzyme Assay |
For non-cell-based receptor binding assays, SB399885 can be evaluated using membrane preparations from cells expressing human recombinant or native 5-HT6 receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-LSD. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled methiothepin. pKi values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human 5-HT6 receptors are cultured in appropriate media. For functional assays, cAMP accumulation is measured as 5-HT6 receptors are Gs-coupled. Cells are treated with various concentrations of SB399885 in the presence of a 5-HT6 receptor agonist such as 5-HT. cAMP levels are measured using ELISA or HTRF-based detection. The compound's ability to inhibit agonist-induced cAMP accumulation is assessed, and IC50 or pKi values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, SB399885 can be administered to rodents via oral gavage or intraperitoneal injection. In models of cognitive function, memory and learning tests such as the Morris water maze or novel object recognition are performed following compound administration. In aged rat models, cognitive performance is assessed. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
SB399885 has a molecular weight of 482.81 and a molecular formula of C18H21Cl2N3O4S·HCl. It is a potent, selective, brain-penetrant and orally active 5-HT6 receptor antagonist. The compound should be stored at -20°C for long-term stability. It is soluble in DMSO and can be formulated for both in vitro and in vivo administration. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of SB399885 has not been extensively reported. As a 5-HT6 receptor antagonist, potential adverse effects may include modulation of serotonergic signaling, which could affect cognition, mood, and appetite. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the central nervous system.
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| References |
[1]. Warren D Hirst, et al. SB-399885 is a potent, selective 5-HT6 receptor antagonist with cognitive enhancing properties in aged rat water maze and novel object recognition models. Eur J Pharmacol. 2006 Dec 28;553(1-3):109-19.
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| Additional Infomation |
SB399885 (CAS 402713-80-8) is a potent, selective, brain-penetrant and orally active 5-HT6 receptor antagonist. It exhibits pKi values of 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. It shows >200-fold selectivity for 5-HT6 over other 5-HT receptors and displays cognitive enhancing properties in aged rat models. It is available for research purposes only.
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| Molecular Formula |
C18H21CL2N3O4S
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| Molecular Weight |
446.35
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| Exact Mass |
445.063
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| CAS # |
402713-80-8
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| Related CAS # |
SB-399885 hydrochloride;402713-81-9
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| PubChem CID |
6918649
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.768
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
600
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C([H])C(=C([H])C(=C1OC([H])([H])[H])N([H])S(C1C([H])=C([H])C(=C(C=1[H])N1C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H])OC([H])([H])[H])(=O)=O)Cl.Cl[H]
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| InChi Key |
ATKZKAYWARYLBW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21Cl2N3O4S/c1-26-17-4-3-13(11-16(17)23-7-5-21-6-8-23)28(24,25)22-15-10-12(19)9-14(20)18(15)27-2/h3-4,9-11,21-22H,5-8H2,1-2H3
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| Chemical Name |
N-(3,5-dichloro-2-methoxyphenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide
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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 | 2.2404 mL | 11.2020 mL | 22.4039 mL | |
| 5 mM | 0.4481 mL | 2.2404 mL | 4.4808 mL | |
| 10 mM | 0.2240 mL | 1.1202 mL | 2.2404 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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