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SKF 83959 hydrobromide
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SKF 83959 hydrobromide图片
CAS NO:67287-95-0
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
SKF83959 hydrobromide 是一种有效的选择性多巴胺D1-like受体部分激动剂。 SKF83959 hydrobromideKi对大鼠D1，D5，D2和 D3的值分别为 1.18, 7.56, 920 和 399 nM。SKF83959 hydrobromide 是一种有效的sigma (σ)-1受体变构调节剂。SKF83959 hydrobromide 属于 benzazepine 家族，对认知功能障碍有改善作用。SKF83959 hydrobromide 可用于研究阿尔茨海默病和抑郁症。
生物活性

SKF83959 hydrobromide is a potent and selective dopamineD1-likereceptor partial agonist. SKF83959 hydrobromideKivalues for ratD1,D5, D2and D3receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator ofsigma (σ)-1receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression[1][2][3][4].

IC50& Target[3][4]

D1Receptor

1.18 nM (Ki)

D5Receptor

7.56 nM (Ki)

D2Receptor

920 nM (Ki)

D3Receptor

399 nM (Ki)

sigma (σ)-1

 

体外研究
(In Vitro)

SKF83959 hydrobromide (10~250 μM) stimulates PIP2 hydrolysis in membranes. SKF83959 hydrobromide (0.1~10 μM; PC12 cell) changes the EC50value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM[2].

体内研究
(In Vivo)

SKF83959 hydrobromide (0.5 and 1 mg/kg; i.p.; 1 hour) reverses the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test[1].
SKF83959 hydrobromide (1 mg/kg; i.p.; 30 minutes) induced memory enhancing effects are prevented by brain-derived neurotrophic factor system blockade[1].
SKF83959 hydrobromide has anti-amnesic activities and restores the scopolamine-decreased BDNF signaling pathway in the hippocampus in mice[1].

Animal Model:Male ICR male mice (8 weeks)[1]
Dosage:0.5 and 1 mg/kg
Administration:I.p.; 1 hour
Result:Reversed the scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test.
Animal Model:Male ICR male mice (8 weeks)[1]
Dosage:1 mg/kg
Administration:I.p.; 30 minutes
Result:The memory enhancing effects were prevented by BDNF system blockade.
分子量

398.72

性状

Solid

Formula

C18H21BrClNO2

CAS 号

67287-95-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 20 mg/mL(50.16 mM;Need ultrasonic and warming)

DMF : 20 mg/mL(50.16 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5080 mL12.5401 mL25.0803 mL
5 mM0.5016 mL2.5080 mL5.0161 mL
10 mM0.2508 mL1.2540 mL2.5080 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。