SB 271046 Hydrochloride

(Synonyms: SB 271046A)
目录号: PL04000 纯度: ≥98%
SB 271046 Hydrochloride (SB 271046A) 是一种高效、选择性和具有口服活性的 5-HT6 受体拮抗剂,对大鼠、猪和人的 pKi 分别为 9.02、8.55 和 8.81。SB 271046 Hydrochloride 对 5-HT6 受体、结合位点和离子通道的选择性超过 200 倍。具有抗惊厥活性 (EC50=0.16 μM)。
CAS No. :209481-24-3
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PL04000-10mg 10mg ¥474.00 请登录
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PL04000-200mg 200mg 询价 询价
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中文名称
SB 271046 Hydrochloride
中文别名
5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[b]噻吩-2-磺胺盐酸盐;5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[B]噻吩-2-磺酰胺盐酸盐;SB 271046 (Hydrochloride);5-氯-N-[4-甲氧基-3-(1-哌嗪基)苯基]-3-甲基苯并[b]噻吩-2-磺酰胺盐酸盐
英文名称
SB 271046 Hydrochloride
英文别名
Benzo[b]thiophene-2-sulfonamide, 5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-, monohydrochloride;5-CHLORO-3-METHYL-BENZO[B]THIOPHENE-2-SULFONIC ACID (4-METHOXY-3-PIPERAZIN-1-YL-PHENYL)-AMIDE HYDROCHLORIDE;Benzo[b]thiophene-2-sulfonamide, 5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-, monohydrochloride;Benzo[b]thiophene-2-sulfonamide, 5-chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methyl-, mon...;SB 271046 hydrochloride;SB271046A;5-chloro-N-(4-methoxy-3-piperazin-1-ylphenyl)-3-methyl-1-benzothiophene-2-sulfonamide hydrochloride;SB-271046;SB-271046A;5-Chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzo-thiophenesulfonamide hydrochloride;5-Chloro-N-[4-methoxy-3-(1-piperazinyl)phenyl]-3-methylbenzo[b]thiophene-2-sulfonamide hydrochloride;SB 271046 (Hydrochloride);SB 271046A
Cas No.
209481-24-3
分子式
C20H22N3O3S2Cl.HCl
分子量
488.45
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述
SB 271046 Hydrochloride (SB 271046A) 是一种高效、选择性和具有口服活性的 5-HT6 受体拮抗剂,对大鼠、猪和人的 pKi 分别为 9.02、8.55 和 8.81。SB 271046 Hydrochloride 对 5-HT6 受体、结合位点和离子通道的选择性超过 200 倍。具有抗惊厥活性 (EC50=0.16 μM)。
产品详情
SB 271046 Hydrochloride (SB 271046A) 是一种高效、选择性和具有口服活性的 5-HT6 受体拮抗剂,对大鼠、猪和人的 pKi 分别为 9.02、8.55 和 8.81。SB 271046 Hydrochloride 对 5-HT6 受体、结合位点和离子通道的选择性超过 200 倍。具有抗惊厥活性 (EC50=0.16 μM)。
生物活性
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pK i of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC 50 =0.16 μM).
性状
Solid
IC50 & Target[1][2]
5-HT6 Receptor 8.92-9.02 (pKi) 5-HT1D Receptor
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Routledge C, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000;130(7):1606-1612.
溶解度数据
In Vitro: DMSO : 50 mg/mL (102.36 mM; Need ultrasonic)H2O : 1 mg/mL (2.05 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)
[1]. Routledge C, et al. Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000;130(7):1606-1612.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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