货号	规格	价格	上海	北京	珠海	重庆	武汉
S89157-5mg买3赠1	99.60%	￥960.00 S89157-5mg ￥960.00 现货（买3赠1）	5 5	-	-	-	-
S89157-10mg促销	99.60%	￥1440.00 ￥1150.00 S89157-10mg ￥1150.00 现货	5 5	-	-	-	-
S89157-25mg促销	99.60%	￥2800.00 ￥2240.00 S89157-25mg ￥2240.00 现货	5 5	-	-	-	-
S89157-100mg促销	≥98%	￥6680.00 ￥5340.00 S89157-100mg ￥5340.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.

靶点：

GABAB receptor;GABAReceptor

体外研究：

In the presence of 10 µM GABA, SSD114 hydrochloride at 25 µM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride, added at 15 and 30 µM, induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 µM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 µM, reaching 161±5.09% over the basal value.

体内研究：

The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, P<0.005]. Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81, P<0.005]. Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice.

参考文献：

1. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.578 ml	12.892 ml	25.784 ml
5 mM	0.516 ml	2.578 ml	5.157 ml
10 mM	0.258 ml	1.289 ml	2.578 ml
50 mM	0.052 ml	0.258 ml	0.516 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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