2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor 5-HT Receptor Adenylate Cyclase
  4. SKF-83566

SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.

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SKF-83566

SKF-83566 構造式

CAS 番号 : 99295-33-7

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 104 在庫あり
Solution
10 mM * 1 mL in DMSO USD 104 在庫あり
Solid
5 mg $95 在庫あり
10 mg $150 在庫あり
25 mg $270 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

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Based on 2 publication(s) in Google Scholar

Other Forms of SKF-83566:

SKF-83566 関連抗体

Top Publications Citing Use of Products

Dopamine Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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  • 純度とドキュメンテーション

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製品説明

SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM)[1][3]. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM[2]. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta[4]. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation[5].

IC50 & Target[1]

D1 Receptor

 

D5 Receptor

 

5-HT2 Receptor

11 nM (Ki)

体外実験

SKF-83566 (0.1 μM-10 μM) causes a concentration-dependent increase in peak evoked extracellular DA concentration ([DA]o)?evoked by single-pulse stimulation, with a maximum 65% increase in peak evoked [DA]o with 5 μM. The EC50 value of this effect of SKF-83566 is 1.3 μM[2].
SKF-83566 inhibited [3H]DA uptake with an IC50?of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [3H]CFT, with an IC50?of 0.51 μM in [3H]DA uptake and [3H]CFT binding studies[2].
Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [3H]CFT binding with an IC50?of 0.77 μM in LLc-PK-rDAT cell membrane preparations[2].

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

SKF-83566 関連抗体
体内実験

SKF 83566 (oral administration; 20 μg/mL; 7 days) alone has no effects on altering LTP (115%). However, combinnation of SKF 83566 and nicotine significantly blocks the enhancement of long-term synaptic potentiation (LTP) induced by pretreatment with nicotine (SKF 83566+nicotine+cocaine, 120%; nicotine+cocaine, 143%)[1].

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

Animal Model: Male C57BL6/J mice (6- to 9-wk-old)[1]
Dosage: 20 µg/mL (Together with nicotine for 7 d, followed by the injection of cocaine)
Administration: Oral administration; 7 days
Result: Blocked nicotine and cocaine-induced facilitation of LTP.
分子量

332.23

分子式

C17H18BrNO
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=C(Br)C=C2CCN(C)CC(C3=CC=CC=C3)C2=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 33.33 mg/mL (100.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0100 mL 15.0498 mL 30.0996 mL
5 mM 0.6020 mL 3.0100 mL 6.0199 mL
10 mM 0.3010 mL 1.5050 mL 3.0100 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.86%

COA (255 KB) HNMR (225 KB) LCMS (117 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0100 mL 15.0498 mL 30.0996 mL 75.2491 mL
5 mM 0.6020 mL 3.0100 mL 6.0199 mL 15.0498 mL
10 mM 0.3010 mL 1.5050 mL 3.0100 mL 7.5249 mL
15 mM 0.2007 mL 1.0033 mL 2.0066 mL 5.0166 mL
20 mM 0.1505 mL 0.7525 mL 1.5050 mL 3.7625 mL
25 mM 0.1204 mL 0.6020 mL 1.2040 mL 3.0100 mL
30 mM 0.1003 mL 0.5017 mL 1.0033 mL 2.5083 mL
40 mM 0.0752 mL 0.3762 mL 0.7525 mL 1.8812 mL
50 mM 0.0602 mL 0.3010 mL 0.6020 mL 1.5050 mL
60 mM 0.0502 mL 0.2508 mL 0.5017 mL 1.2542 mL
80 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9406 mL
100 mM 0.0301 mL 0.1505 mL 0.3010 mL 0.7525 mL
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SKF-83566 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SKF-8356699295-33-7SKF83566SKF 83566Dopamine Receptor5-HT ReceptorAdenylate CyclaseSerotonin Receptor5-hydroxytryptamine ReceptorAdenylyl cyclasedentate gyrusDGhippocampusdrug-relatedassociative memorydopamine uptakedorsal striatumparkinson’s diseasenicotine cravingInhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-103430A
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