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SB-649868

Name: SB-649868
Brand: TargetMol
SKU: T5498
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5498Cas No. 380899-24-1

Alias GSK649868

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).

SB-649868

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Purity: 99.53%

Catalog No. T5498Alias GSK649868Cas 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).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$31	In Stock	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$118	In Stock	In Stock
25 mg	$251	In Stock	In Stock
50 mg	$407	In Stock	In Stock
100 mg	$653	In Stock	In Stock
200 mg	$876	-	In Stock
1 mL x 10 mM (in DMSO)	$83	In Stock	In Stock

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

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Purity:99.53%

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COA LCMS HNMR

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).
Targets&IC50	OX1:9.4 (pKi), OX2:9.5 (pKi)
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
Synonyms	GSK649868

Chemical Properties

Molecular Weight	477.55
Formula	C₂₆H₂₄FN₃O₃S
Cas No.	380899-24-1
Smiles	Cc1nc(C(=O)N2CCCC[C@H]2CNC(=O)c2cccc3occc23)c(s1)-c1ccc(F)cc1
Relative Density.	1.305 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 100 mg/mL (209.4 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.38 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

	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)

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% 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 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 μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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