SR 57227 hydrochloride|77145-61-0|-陌孚医药/Medlife

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SR 57227 hydrochloride

目录号: PC11132 纯度: ≥98%

CAS No. :77145-61-0

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中文名称	SR 57227 hydrochloride
中文别名	SR57227盐酸盐;4-氨基-1-(6-氯-2-吡啶基)哌啶盐酸盐
英文名称	SR 57227 hydrochloride
英文别名	SR 57227 HYDROCHLORIDE;[1-(6-chloropyridin-2-yl)piperidin-4-yl]amine hydrochloride;1-(6-chloropyridin-2-yl)piperidin-4-amine,hydrochloride;SR 57,227A;4-amino-1-(6-chloro-2-pyridyl)-piperidine hydrochloride
Cas No.	77145-61-0
分子式	C₁₀H₁₄N₃Cl^.HCl
分子量	248.15
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC₅₀) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
性状	Solid
体外研究(In Vitro)	SR 57227A binds to 5-HT3 receptors labelled with [3H]S-zacopride with an affinity (K_i) of 115 nM in rat cerebral cortex, 150 nM in NG 108-15 cell membranes and 103 nM in whole NG 108-15 cell. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	SR 57227A (1-30 mg/kg; i.p.) dose-dependently reduces immobility time in the forced swimming test with an ED₅₀ value for this effect of 14.2 mg/kg. In the forced swimming test, SR 57227A dose-dependently reduces the duration of immobility in rats after i.p. administration. (ED₅₀=7.6 mg/kg i.p. in rats.) SR 57227A is also active in both species after oral administration. In a time-course study in mice, SR 57227A (20 mg/kg p.o.) produces a significant effect lasting 6 hours. SR 57227A (1 and 3 mg/kg i.p.) reduces the elevation of the escape failures in the learned helplessness model in rats by 50-60% on the last two days of the avoidance task, and reduces isolation-induced aggressivity in mice by 50 to 85%, an effect which is antagonised by Zacopride (1 mg/kg i.p.). Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
储存方式	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Poncelet M, et al, Le Fur G. Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents. J Neural Transm Gen Sect. 1995;102(2):83‐90. [Information] [2]. Bachy A, et al. SR 57227A: a potent and selective agonist at central and peripheral 5-HT3 receptors 体外研究 and in vivo. Eur J Pharmacol. 1993;237(2-3):299‐309. [Information]

溶解度数据

体外研究:

H₂O : 33.33 mg/mL (134.31 mM; Need ultrasonic)

DMSO : 8.33 mg/mL (33.57 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0298 mL	20.1491 mL	40.2982 mL
5 mM	0.8060 mL	4.0298 mL	8.0596 mL
10 mM	0.4030 mL	2.0149 mL	4.0298 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 10 mg/mL (40.30 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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产品使用指南

Data Sheet

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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