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| | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride Basic information |
| Product Name: | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride | | Synonyms: | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride;SB 271046A;Benzo[b]thiophene-2-sulfonaMide, 5-chloro-N-[4-Methoxy-3-(1-piperazinyl)phenyl]-3-Methyl-, Monohydrochloride;5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzo-thiophenesulfonamide hydrochloride;4-[(3-chloro-1,4-dioxonaphthalen-2-yl)amino]benzenesulfonamide;SB 271046A; SB-271046A;SB-271046A >=98% (HPLC);SB 271046 HCl (SB-271046A) | | CAS: | 209481-24-3 | | MF: | C20H23Cl2N3O3S2 | | MW: | 488.44 | | EINECS: | | | Product Categories: | | | Mol File: | 209481-24-3.mol | ![5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride Structure](CAS/GIF/209481-24-3.gif) |
| | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMSO: >20mg/mL | | form | powder | | color | White to light brown | | InChI | 1S/C20H22ClN3O3S2.ClH/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;1H | | InChIKey | RMXZRJYGJMSDQK-UHFFFAOYSA-N | | SMILES | Cl.COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N4CCNCC4 |
| WGK Germany | nwg | | Storage Class | 11 - Combustible Solids |
| | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride Usage And Synthesis |
| Uses | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophene-2-sulfonamide Hydrochloride is a 5-Hydroxytryptamine6 receptor antagonist. | | Biological Activity | The first potent and selective 5-HT6 antagonist. Training in cognitive tasks, as well as administration SB-271046, induces an increase in pERK1/2 and pCREB1 levels, while CREB2 levels are significantly reduced; cognition-enhancing properties of SB-271046 are attributed to the effect on pERK1/2, not pCREB1/2. SB-271046 reverses MK-801-induced, but not scopolamine-induced, learning impairments. However, with coadministration of galanthamine, both types of learning impairments were ameliorated. | | in vivo | SB 271046 Hydrochloride (10mg/kg; p.o.) produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of 0.1mg/kg p.o. and maximum effect at 4h post-dose[1]. | Animal Model: | Male Sprague Dawley rats[1] | | Dosage: | 10mg/kg | | Administration: | P.o. | | Result: | Produced an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of 0.1mgkg1 p.o. and maximum effect at 4h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB-271046 (EC50 of 0.16μM) and brain concentrations of 0.01-0.04μM at Cmax.
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| | IC 50 | 5-HT6 Receptor: 8.92-9.02 (pKi); 5-HT1D Receptor: 6.55 (pKi); 5-HT1A Receptor: 6.35 (pKi); 5-HT1B Receptor: 6.05 (pKi); 5-HT1F Receptor: 5.95 (pKi); 5-HT2A Receptor: 5.62 (pKi); 5-HT2B Receptor: 5.41 (pKi); 5-HT7 Receptor: 5.39 (pKi); 5-HT4 Receptor: 5.27 (pKi); 5-HT1E Receptor: <4.99 (pKi); Human 5-HT2C Receptor: 5.73 (pKi) | | storage | Desiccate at RT |
| | 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride Preparation Products And Raw materials |
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