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SKF-83566

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Purity:95.00%

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COA HNMR

SKF-83566

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

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Pack Size	Price	Availability	Quantity
1 mg	$49	In Stock
1 mL x 10 mM (in DMSO)	$83	In Stock

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Product Introduction

Bioactivity

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
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)

Chemical Properties

Molecular Weight	332.23
Formula	C17H18BrNO
Cas No.	99295-33-7

Storage & Solubility Information

Storage

store at low temperature|Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0100 mL	15.0498 mL	30.0996 mL	150.4981 mL
5 mM	0.6020 mL	3.0100 mL	6.0199 mL	30.0996 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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