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SB-674042

Name: SB-674042
Brand: TargetMol
SKU: T16854
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16854Cas No. 483313-22-0

Alias SB674042

SB-674042 is a potent, selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50 values of 3.76 nM and 531 nM, respectively. SB-674042 is suitable for the treatment of depression.

SB-674042

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Purity: 99.9%

Catalog No. T16854Alias SB674042Cas No. 483313-22-0

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$45	-	In Stock
1 mL x 10 mM (in DMSO)	$94	-	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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Purity:99.9%

Appearance:Solid

Color:White to Yellow

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COA LCMS

Product Introduction

Bioactivity

Description	SB-674042 is a potent, selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50 values of 3.76 nM and 531 nM, respectively. SB-674042 is suitable for the treatment of depression.
Targets&IC50	OX1 receptor:3.76 nM, OX1 receptor:1.1 nM (Ki), OX2 receptor:129 nM (Ki), OX2 receptor:531 nM
In vitro	[(3)H]SB-674042 is a specific, high-affinity radioligand for the OX(1) receptor. Specific binding of [(3)H]SB-674042 was saturable in both whole cell and membrane formats. Analyses suggested a single high-affinity site, with K(d) values of 3.76+/-0.45 and 5.03+/-0.31 nM[1]。Treatment of cells co-expressing the orexin-1 and CB1 receptors with the orexin-1 receptor antagonist SB-674042 also resulted in re-localization of both receptors to the cell surface. Treatment with SB-674042 also reduced the potency of a CB1 receptor agonist to phosphorylate ERK1/2 only when the two receptors were co-expressed[4].
In vivo	In the Stress Alternatives Model (SMA) in mice, administration of SB-674042 at a dose of 0.3 nM/0.3 μL via icv (intracerebroventricular injection) reduces contextual and cue fear freezing responses in Stay animals[2].
Synonyms	SB674042

Chemical Properties

Molecular Weight	448.51
Formula	C₂₄H₂₁FN₄O₂S
Cas No.	483313-22-0
Smiles	Cc1nc(C(=O)N2CCC[C@H]2Cc2nnc(o2)-c2ccccc2)c(s1)-c1ccccc1F
Relative Density.	1.326 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: 20 mg/mL (44.59 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.23 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	2.2296 mL	11.1480 mL	22.2960 mL	111.4802 mL
5 mM	0.4459 mL	2.2296 mL	4.4592 mL	22.2960 mL
10 mM	0.2230 mL	1.1148 mL	2.2296 mL	11.1480 mL
20 mM	0.1115 mL	0.5574 mL	1.1148 mL	5.5740 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