1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
    Sigma Receptor
  3. SKF 83959 hydrobromide

SKF 83959 hydrobromide 

目录号: HY-103412 纯度: 99.86%
产品使用指南

SKF83959 hydrobromide 是一种有效的选择性多巴胺 D1-like 受体部分激动剂 (大鼠D1, D5, D2 和 D3 受体 Ki 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。

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SKF 83959 hydrobromide Chemical Structure

SKF 83959 hydrobromide Chemical Structure

CAS No. : 67287-95-0

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规格 价格 是否有货 数量
5 mg ¥6300 In-stock
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50 mg   询价  

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  • 生物活性

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  • 参考文献

生物活性

SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist (Ki values are 1.18, 7.56, 920 and 399 nM for rat D1, D5, D2 and D3 receptors, respectively). SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. 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]

D1 Receptor

1.18 nM (Ki)

D5 Receptor

7.56 nM (Ki)

D2 Receptor

920 nM (Ki)

D3 Receptor

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 EC50 value of SKF81297 from 0.5 nM in control tissue to 31.6 nM, 251.2 nM and 631.0 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR male mice (8 weeks)
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)
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

Formula

C₁₈H₂₁BrClNO₂

CAS 号
SMILES

OC1=C(O)C=C2C(C3=CC=CC(C)=C3)CN(C)CCC2=C1Cl.[H]Br

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

Keywords:

SKF 83959SKF83959SKF-83959Dopamine ReceptorSigma ReceptorPC12PIP2hydrolysisdopaminebenzazepinecognitivedysfunctionAlzheimerInhibitorinhibitorinhibit

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SKF 83959 hydrobromide
目录号:
HY-103412
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