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GSK1059865

Name: GSK1059865
Brand: TargetMol
SKU: T11477
Price: 66 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11477Cas No. 1191044-58-2

Alias GSK-1059865, GSK 1059865

GSK1059865 is a highly selective orexin-1 receptor antagonist that significantly reduces voluntary ethanol intake in ethanol-dependent mice following chronic intermittent ethanol exposure, producing dose-dependent suppression of alcohol consumption without affecting sucrose intake, while exhibiting minimal effects in non-dependent controls except at high doses, thereby highlighting its utility for investigating orexin signaling in alcohol dependence and addictive behaviors.

GSK1059865

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Catalog No. T11477Alias GSK-1059865, GSK 1059865Cas No. 1191044-58-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$66	-	In Stock
5 mg	$158	-	In Stock
10 mg	$255	-	In Stock
1 mL x 10 mM (in DMSO)	$176	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Appearance:Solid

Color:Yellow

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COA

Product Introduction

Bioactivity

Description	GSK1059865 is a highly selective orexin-1 receptor antagonist that significantly reduces voluntary ethanol intake in ethanol-dependent mice following chronic intermittent ethanol exposure, producing dose-dependent suppression of alcohol consumption without affecting sucrose intake, while exhibiting minimal effects in non-dependent controls except at high doses, thereby highlighting its utility for investigating orexin signaling in alcohol dependence and addictive behaviors.
Targets&IC50	OX1 receptor:8.77 (pKb)
In vitro	In receptor assays, GSK1059865 acted as an Orexin-1 (OX1) receptor antagonist with a pKB of 8.77. At low concentrations (0.3-10 nM), it functioned as an insurmountable antagonist suppressing the maximal Orexin-A response, whereas at higher concentrations (0.1-3.3 μM), it exhibited a surmountable profile characterized by a parallel rightward shift of the EC50 [1].
In vivo	In ethanol-dependent mice (CIE model), GSK1059865 reduced ethanol consumption in a dose-dependent manner. In control mice (air-exposed), consumption was only affected at the highest dose tested. The compound showed no effect on sucrose intake. In rat fMRI studies, intraperitoneal administration of GSK1059865 inhibited the relative cerebral blood volume (rCBV) response induced by Yohimbine in specific brain regions. Pretreatment with the compound was associated with a baseline mean arterial blood pressure higher than that of the control group [1][3].
Synonyms	GSK-1059865, GSK 1059865

Chemical Properties

Molecular Weight	436.32
Formula	C₂₀H₂₃BrFN₃O₂
Cas No.	1191044-58-2
Smiles	C(=O)(N1[C@H](CNC2=CC=C(Br)C=N2)CC[C@H](C)C1)C3=C(OC)C(F)=CC=C3
Relative Density.	1.376 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 160 mg/mL (366.7 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2919 mL	11.4595 mL	22.9190 mL	114.5948 mL
5 mM	0.4584 mL	2.2919 mL	4.5838 mL	22.9190 mL
10 mM	0.2292 mL	1.1459 mL	2.2919 mL	11.4595 mL
20 mM	0.1146 mL	0.5730 mL	1.1459 mL	5.7297 mL
50 mM	0.0458 mL	0.2292 mL	0.4584 mL	2.2919 mL
100 mM	0.0229 mL	0.1146 mL	0.2292 mL	1.1459 mL

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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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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