目錄:MedChemExpress LLC>>信號(hào)通路>> SB 271046 Hydrochloride | MedChemExpress (MCE)
| 參考價(jià) | ￥ 741 |
| 參考價(jià) | ￥ 741 |
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| CAS | 209481-24-3 | 純度 | 99.21% |
|---|---|---|---|
| 分子量 | 488.45 | 分子式 | C??H??Cl?N?O?S? |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號(hào) | HY-14336A | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥/生物制藥 |
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CAS No. : 209481-24-3
MCE 國(guó)際站：SB 271046 Hydrochloride
產(chǎn)品活性：SB 271046 Hydrochloride (SB 271046A) 是一種高效、選擇性和具有口服活性的 5-HT6 受體拮抗劑，對(duì)大鼠、豬和人的 pKi 分別為 9.02、8.55 和 8.81。SB 271046 Hydrochloride 對(duì) 5-HT6 受體、結(jié)合位點(diǎn)和離子通道的選擇性超過(guò) 200 倍。具有抗驚厥活性 (EC50=0.16 μM)。
研究領(lǐng)域：GPCR/G Protein | Neuronal Signaling
作用靶點(diǎn)：5-HT Receptor
In Vitro: SB 271046 Hydrochloride (SB 271046A) shows pKi values of 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively. SB-271046 Hydrochloride competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71.
In Vivo: SB 271046 Hydrochloride (10?mg/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 ?0.1?mg/kg p.o. and maximum effect at 4?h post-dose.
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