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| | Sb-742457 Basic information |
| Product Name: | Sb-742457 | | Synonyms: | Gsk 742457;Sb 742457;Sb-742457;3-Phenylsulfonyl-8-(piperazin-1-yl)quinoline;SB 742457/GSK 742457;Quinoline, 3-(phenylsulfonyl)-8-(1-piperazinyl)-;SB742457:Intepirdine;Intepirdine(SB742457) | | CAS: | 607742-69-8 | | MF: | C19H19N3O2S | | MW: | 353.44 | | EINECS: | | | Product Categories: | Inhibitors;API | | Mol File: | 607742-69-8.mol |  |
| | Sb-742457 Chemical Properties |
| Boiling point | 608.3±45.0 °C(Predicted) | | density | 1.292 | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; ≥17.65 mg/mL in DMSO; ≥2.13 mg/mL in EtOH with gentle warming and ultrasonic | | form | solid | | pka | 8?+-.0.10(Predicted) |
| | Sb-742457 Usage And Synthesis |
| Description | SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM). SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity. SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells. In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine in rats. It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management. | | Uses | SB 742457 is a selective 5-HT6 receptor antagonist which is known to be involved in improving cognitive function. | | target | 5-HT6 | | references | [1] aaron t. t. chuang, andrew foley, perdita l. pugh, david sunter, xin tong, ciaran regan, lee a. dawson, andrew d. medhurst, neil upton.5-ht6 receptor antagonist sb-742457 as a novel cognitive enhancing agent for alzheimer’s disease. alzheimer's & dementia: the journal of the alzheimer's association volume 2, issue 3, supplement, pages s631–s632, july 2006 |
| | Sb-742457 Preparation Products And Raw materials |
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