SKF 83959 hydrobromide

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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。

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 hydrobromideK_i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 hydrobromideK_ivalues 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 mg

5 mg

10 mg

1 mM	2.5080 mL	12.5401 mL	25.0803 mL
5 mM	0.5016 mL	2.5080 mL	5.0161 mL
10 mM	0.2508 mL	1.2540 mL	2.5080 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。