SB271046
SB271046 Basic information
- Product Name:
- SB271046
- Synonyms:
-
- 5-chloro-N-(4-methoxy-3-(piperazin-1-yl)phenyl)-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride
- 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-benzo[b]thiophen-2-sulfonamide hydrochloride
- SB 271046 hydrochloride
- 5-Chloro-3-Methyl-Benzo[b]Thiophene-2-Carboxylic Acid (4-Methoxy-3-Piperazin-1-yl-Phenyl)-AMide H
- 1. 5-Chloro-3-Methyl-Benzo[b]Thiophene-2-Carboxylic Acid (4-Methoxy-3-Piperazin-1-yl-Phenyl)-AMide H
- SB 271046
- 5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide
- SB 737050
- CAS:
- 209481-20-9
- MF:
- C20H22ClN3O3S2
- MW:
- 451.99
- Product Categories:
-
- Inhibitors
- Mol File:
- 209481-20-9.mol
SB271046 Chemical Properties
- Melting point:
- 240-241℃ (DEC.)
- Boiling point:
- 664.3±65.0 °C(Predicted)
- Density
- 1.400
- storage temp.
- Desiccate at RT
- solubility
- Soluble in DMSO > 10 mM
- form
- Powder
- pka
- 7.61±0.50(Predicted)
SB271046 Usage And Synthesis
Uses
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pKi of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity[1].
in vivo
SB 271046 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 ?0.1?mg/kg p.o. and maximum effect at 4?h post-dose. The level of anticonvulsant activity achieved correlated well with the blood concentrations of SB 271046 (EC50 of 0.16?μM) and brain concentrations of 0.01-0.04?μM at Cmax[1].
IC 50
5-HT6 Receptor: 8.92-9.09 (pKi)
storage
room temperature (desiccate)
References
[1] C Routledge, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000 Aug;130(7):1606-12. DOI:10.1038/sj.bjp.0703457
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