中文名称: SX-3228
英文名称: SX-3228
CAS No: 156364-04-4
分子式: C18H18N4O3
分子量: 338.36
S10951 SX-3228 (psaitong)
包装规格:
5mg in glass bottle
产品描述:

基本信息

产品编号:

S10951

产品名称:

SX-3228

CAS:

156364-04-4

 

储存条件

粉末

-20℃

四年

分子式:

C18H18N4O3

溶于液体

-80℃

二年

分子量:

338.36

 

 

化学名: 

6-BENZYL-3-(5-METHOXY-1,3,4-OXADIAZOL-2-YL)-1,5,7,8-TETRAHYDRO-1,6-NAPHTHYRIDIN-2-ONE

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

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。

 

生物活性

产品描述

一种选择性苯二氮卓类(benzodiazepine1,BZ1)受体激动剂

靶点

IC50:17nM (BZ1 receptor)

 

体外研究

SX-3228 is a selective ligand for the BZ1 receptor.Among the BZ-receptor subtypes,SX-3228 preferentially binds to the BZ1 receptor (IC50=17nM).It has very weak affinity for the BZ2 receptor (spinal cord: IC50=127nM),and virtually no affinity for the peripheral type BZ receptor (kidney:IC50>10000nM).A compound with similar selectivity,SX-3228 has been shown to bind to BZ receptors,but not to dopamine (D1,D2),serotonin (5-HT1,5-HT2 and 5-HT3 subtypes),noradrenaline (α1,α2,β),GABA or acetylcholine (muscarinic) subtypes.

体内研究

Administration of 0.5-2.5mg/kg SX-3228 to rats during the light phase induces a significant reduction of rapid-eyemovement sleep (REMS) (P<0.05) during the third recording hour.Administration of SX-3228 (0.5-2.5mg/kg) at the beginning of the dark period significantly and dose-dependently reduces waking (W) and increases slow wave sleep (SWS) during the 6-h recording period (P<0.05-0.01);however,significant changes during the last recording hour are restricted to the 2.5mg/kg dose (P<0.01).

 

推荐实验方法(仅供参考)

动物实验:

 

Rats

Twelve male Wistar rats (350-380g) are used.Subcutaneous (sc) injections are given in a final volume of 1.0mL/kg.All rats are given the corresponding volume of control solution (saline+Tween-80) in the control sessions. Following sc injection,a 6-h sleep recording is started at approximately 8:00 a.m.At least 4 days are allowed to elapse between injections to avoid long-lasting and rebound effects on sleep.The effects of SX-3228 0.5-2.5mg/kg are studied in one group of animals (N=6) during the light phase of the 12-h light:12-h dark cycle,starting 1h after the beginning of the light period.Polysomnographic recordings are started immediately after control solution or drug administration. Each rat receives all four treatments (control,and 0.5,1.0,2.5mg/kg SX-3228).

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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