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Chemical Structure : SB-271046
CAS No.: 209481-20-9
Catalog No.: PC-21121Not For Human Use, Lab Use Only.
SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist, potently displaces [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT6 receptors recombinantly expressed in HeLa cells with pKi 8.92 and 9.09 respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $98 | In stock | |
| 25 mg | $168 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | $428 | In stock | |
| 250 mg | Get quote |
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SB-271046 is a potent, selective and orally active 5-HT6 receptor antagonist, potently displaces [(3)H]-LSD and [(125)I]-SB-258585 from human 5-HT6 receptors recombinantly expressed in HeLa cells with pKi 8.92 and 9.09 respectively.
SB-271046 also displaces [(125)I]-SB-258585 from human caudate putamen and rat and pig striatum membranes (pK(i) 8.81, 9.02 and 8.55 respectively).
SB-271046 is >200 fold selective for the 5-HT(6) receptor vs. 55 other receptors, binding sites and ion channels.
SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA(2) of 8.71 in functional studies on human 5-HT(6) receptors.
SB-271046 (10 mg/kg) demonstrates anticonvulsant activity in the rat MEST test.
| M.Wt | 488.44 | |
| Formula | C20H23Cl2N3O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
5-Chloro-3-methyl-benzo[b]thiophene-2-sulphonic acid (4-methoxy-3-piperazin-1-yl-phenyl)-amide monohydrochloride |
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1. C Routledge, et al. Br J Pharmacol. 2000 Aug;130(7):1606-12.
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