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GSK1059865

Name: GSK1059865
Brand: TargetMol
SKU: T11477
Rating: 4.5 (1 reviews)

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Catalog No. T11477Cas No. 1191044-58-2

GSK1059865 is a potent antagonist of the orexin 1 receptor.

GSK1059865

😃Good

Catalog No. T11477Cas No. 1191044-58-2

GSK1059865 is a potent antagonist of the orexin 1 receptor.

Pack Size	Price	Availability
2 mg	$108	6-8 weeks
25 mg	$736	6-8 weeks
50 mg	$956	6-8 weeks
100 mg	$1,690	6-8 weeks

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Product Introduction

Bioactivity

Description

GSK1059865 is a potent antagonist of the orexin 1 receptor.

In vivo

GSK1059865 (0.3?nM-10?nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC50 and a concomitant decrease of the agonist maximal response.?The calculated pKB value is 8.77±0.12 for GSK1059865.?GSK1059865 (0.1-3.3?μM) produces a classical surmountable profile with parallel rightward shift of the OXA EC50 without depression of the agonist maximal response.?Intraperitoneal administration of GSK1059865 produces a region-dependent inhibition of yohimbine-induced relative cerebral blood volume response.?The administration of GSK1059865 per se produces a weak relative cerebral blood volume increase in several brain regions.?GSK1059865-pretreated animals exhibit slightly higher baseline mean arterial blood pressure values than controls.Treatment with GSK1059865 significantly decreases ethanol drinking in a dose-dependent manner in CIE-exposed mice.?In contrast GSK1059865 decreases drinking in air-exposed mice only at the highest dose used.?There is no effect of GSK1059865 on sucrose intake.

Chemical Properties

Molecular Weight	436.32
Formula	C₂₀H₂₃BrFN₃O₂
Cas No.	1191044-58-2
Relative Density.	1.376 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 50 mg/mL (114.59 mM)

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 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 . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

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

(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 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

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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

Keywords

Orexin 1 receptorGSK-1059865GSK1059865GSK 1059865