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SB-649868

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Purity:99.58%

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COA HNMR HPLC

SB-649868

Catalog No. T5498Cas No. 380899-24-1

SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

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Pack Size	Price	Availability
1 mg	$48	In Stock
5 mg	$113	In Stock
10 mg	$197	In Stock
25 mg	$419	In Stock
50 mg	$679	In Stock
100 mg	$1,090	In Stock
1 mL x 10 mM (in DMSO)	$138	In Stock

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Product Introduction

Bioactivity

Description	SB-649868 (GSK649868) is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).
In vitro	SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67;?OX2=9.64).?SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27;?OX2=8.91.?Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior.?The calculated apparent pKb values are 9.67 0.03 and 9.64 0.07 for OX1 and OX2
Alias	GSK649868

Chemical Properties

Molecular Weight	477.55
Formula	C26H24FN3O3S
Cas No.	380899-24-1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (209.40 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0940 mL	10.4701 mL	20.9402 mL	104.7011 mL
5 mM	0.4188 mL	2.0940 mL	4.1880 mL	20.9402 mL
10 mM	0.2094 mL	1.0470 mL	2.0940 mL	10.4701 mL
20 mM	0.1047 mL	0.5235 mL	1.0470 mL	5.2351 mL
50 mM	0.0419 mL	0.2094 mL	0.4188 mL	2.0940 mL
100 mM	0.0209 mL	0.1047 mL	0.2094 mL	1.0470 mL

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In Vivo Formulation Calculator (Clear solution)

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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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