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SKF-83566
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Catalog No. T8702Cas No. 99295-33-7
SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM
SKF-83566
🥰Excellent
Purity: 99.82%
Catalog No. T8702Cas No. 99295-33-7
SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $48 | In Stock | |
| 5 mg | $77 | In Stock | |
| 10 mg | $123 | In Stock | |
| 25 mg | $222 | In Stock | |
| 50 mg | $328 | In Stock | |
| 100 mg | $492 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $83 | In Stock |
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Purity:99.82%
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Product Introduction
Bioactivity
Chemical Properties
| Description | SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM |
| Targets&IC50 | 5-HT2 receptor:11 nM (Ki) |
| In vitro | SKF-83566 caused a concentration-dependent increase in peak single-pulse evoked extracellular DA concentration, with a maximum increase of 65% in 5 μM SKF-83566.?This was accompanied by a concentration-dependent increase in extracellular DA concentration clearance time.?Both effects were occluded by nomifensine (1 μM), a dopamine transporter (DAT) inhibitor, suggesting that SKF-83566 acted via the DAT.?Tested this by examining [(3)H]DA uptake into LLc-PK cells expressing rat DAT, and confirmed that SKF-83566 is a competitive DAT inhibitor with an IC(50) of 5.7 μM.?Binding studies with [(3)H]CFT, a cocaine analog, showed even more potent action of SKF-83566 at the DAT cocaine binding site (IC(50) = 0.51 μM)[1]. |
| In vivo | The facilitation induced by nicotine and cocaine can be blocked by oral administration of the dopamine D1/D5 receptor antagonist (SKF 83566) |
| Molecular Weight | 332.23 |
| Formula | C17H18BrNO |
| Cas No. | 99295-33-7 |
| Smiles | CN1CCc2cc(Br)c(O)cc2C(C1)c1ccccc1 |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mM, Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.02 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
SKF-83566SKF83566SKF 83566Serotonin Receptorparkinson's diseasenicotine cravingInhibitorinhibithippocampusdrug-relateddorsal striatumDopamineReceptordopamine uptakeDopamine ReceptorDopaminedentate gyrusD5D1associative memoryAdenylyl cyclaseAdenylate Cyclase5-hydroxytryptamine Receptor5HTReceptor5-HT25-HT Receptor5HT Receptor
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