Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
SB271046 (SB 271046; SB-271046; SB-271046A; SB271046A) is a novel, potent, selective and orally bioactive 5-HT6 receptor antagonist with important biological activity. It has 200 times more selectivity than other 5-HT receptor subtypes and inhibits 5-HT6 with a pKi of 8.9. Human 5-HT6 receptors that were recombinantly expressed in HeLa cells in vitro were replaced by SB-271046 with [125I]-SB-258585 and [3H]-LSD. Moreover, [125I]-SB-258585 was transferred by SB-271046 from the rat and pig striatum membranes to the human caudate putamen. In HeLa cells that are stable expression hosts of human 5-HT6 receptors, adenylyl cyclase activity is stimulated by 5-HT alone or in response to increasing concentrations of SB-271046 (10, 30, 100, and 300 nM).
Targets |
5-HT6 Receptor ( pKi = 8.92-9.09 )
|
---|---|
ln Vitro |
In vitro activity :SB 271046 competitively inhibited 5-HT-induced stimulation of adenylyl cyclase activity in functional studies on human 5-HT6 receptors, with a pA2 of 8.71[1].
|
ln Vivo |
SB-271046 results in a minimum effective dose of approximately 0.1 mg/kg p.o. and maximum effect at 4 hours post-dose in the rat maximal electroshock seizure threshold (MEST) test. This rises the seizure threshold over a broad dose range. The blood and brain concentrations of SB 271046 (EC50 of 0.16 μM) and Cmax (0.01-0.04 μM) showed a strong correlation with the achieved level of anticonvulsant activity[1].
|
Animal Protocol |
Male Sprague Dawley rats; Dissolved in 1% methyl cellulose in water; 30 mg/kg; Oral gavage
|
References |
Molecular Formula |
C20H22CLN3O3S2
|
---|---|
Molecular Weight |
451.99
|
Exact Mass |
451.08
|
CAS # |
209481-20-9
|
SMILES |
CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4
|
InChi Key |
LOCQRDBFWSXQQI-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C20H22ClN3O3S2/c1-13-16-11-14(21)3-6-19(16)28-20(13)29(25,26)23-15-4-5-18(27-2)17(12-15)24-9-7-22-8-10-24/h3-6,11-12,22-23H,7-10H2,1-2H3
|
Chemical Name |
5-chloro-N-(4-methoxy-3-piperazin-1-ylphenyl)-3-methyl-1-benzothiophene-2-sulfonamide
|
Synonyms |
SB-271046; SB 271046; SB271046; SB-271046 HCl; SB-271046 hydrochloride
|
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 (In Vitro) |
DMSO: ~40 mg/mL (~81.9 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
---|---|
Solubility (In Vivo) |
1% methylcellulose: ~30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2124 mL | 11.0622 mL | 22.1244 mL | |
5 mM | 0.4425 mL | 2.2124 mL | 4.4249 mL | |
10 mM | 0.2212 mL | 1.1062 mL | 2.2124 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.