SB 271046 Hydrochloride SB 271046A|cas:209481-24-3|西域试剂

SB 271046 Hydrochloride SB 271046A,98.64%

产品编号：Bellancom-14336A| CAS NO：209481-24-3| 分子式：C₂₀H₂₃Cl₂N₃O₃S₂| 分子量：488.45

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-14336A		￥1070.00	杭州北京（现货）
Bellancom-14336A		￥4092.00	杭州北京（现货）

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SB 271046 Hydrochloride SB 271046A

产品介绍

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 pK_i 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 (EC₅₀=0.16 μM).

体外研究

SB 271046 Hydrochloride (SB 271046A) shows pK_i 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague Dawley rats
Dosage:	10 mg/kg
Administration:	P.o.
Result:	Produced 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−1 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 C_max.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague Dawley rats
Dosage:	10 mg/kg
Administration:	P.o.
Result:	Produced 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−1 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 C_max.

性状

Solid

溶解性数据

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0473 mL	10.2365 mL	20.4729 mL
5 mM	0.4095 mL	2.0473 mL	4.0946 mL
10 mM	0.2047 mL	1.0236 mL	2.0473 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。