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SB-408124

Name: SB-408124
Brand: TargetMol
SKU: T6658
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6658Cas No. 288150-92-5

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.

SB-408124

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Purity: 99.81%

Catalog No. T6658Cas No. 288150-92-5

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$40	-	In Stock
10 mg	$64	-	In Stock
25 mg	$127	-	In Stock
1 mL x 10 mM (in DMSO)	$59	-	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:99.81%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.
Targets&IC50	OX1 (whole cell):57 nM(Ki), OX1 (membrane):27 nM(Ki)
In vitro	SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. [1] A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production. [2]
In vivo	SB-408124 (30 μg/10 μL, administered intracerebroventricularly) reduces Orexin-A-induced water intake in Wistar rats. Intracerebroventricular Orexin-A (30 μg/10 μL) inhibits vasopressin increase induced by histamine or 2.5% NaCl, and this effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). [3] [4]

Chemical Properties

Molecular Weight	356.37
Formula	C₁₉H₁₈F₂N₄O
Cas No.	288150-92-5
Smiles	CN(C)c1ccc(NC(=O)Nc2cc(C)nc3c(F)cc(F)cc23)cc1
Relative Density.	1.371 g/cm3

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: 62.5 mg/mL (175.38 mM), Sonication and heating are recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (7.02 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	2.8061 mL	14.0304 mL	28.0607 mL	140.3036 mL
5 mM	0.5612 mL	2.8061 mL	5.6121 mL	28.0607 mL
10 mM	0.2806 mL	1.4030 mL	2.8061 mL	14.0304 mL
20 mM	0.1403 mL	0.7015 mL	1.4030 mL	7.0152 mL
50 mM	0.0561 mL	0.2806 mL	0.5612 mL	2.8061 mL
100 mM	0.0281 mL	0.1403 mL	0.2806 mL	1.4030 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