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NBI-74330

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Catalog No. T5644Cas No. 855527-92-3
Alias NBI74330

NBI-74330 is a high-affinity CXCR3 antagonist that inhibits the binding of CXCR3 to its ligands CXCL10 and CXCL11, reduces the formation of atherosclerotic plaques in LDL receptor-deficient mice, and decreases the migration of CD4+ T cells and macrophages to the peritoneum.

NBI-74330

NBI-74330

😃Good
Purity: 99.37%
Catalog No. T5644Alias NBI74330Cas No. 855527-92-3
NBI-74330 is a high-affinity CXCR3 antagonist that inhibits the binding of CXCR3 to its ligands CXCL10 and CXCL11, reduces the formation of atherosclerotic plaques in LDL receptor-deficient mice, and decreases the migration of CD4+ T cells and macrophages to the peritoneum.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$56-In Stock
5 mg$135-In Stock
10 mg$226-In Stock
25 mg$397-In Stock
50 mg$773-In Stock
100 mg$1,230-In Stock
200 mg$1,650-In Stock
1 mL x 10 mM (in DMSO)$179-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:99.37%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
NBI-74330 is a high-affinity CXCR3 antagonist that inhibits the binding of CXCR3 to its ligands CXCL10 and CXCL11, reduces the formation of atherosclerotic plaques in LDL receptor-deficient mice, and decreases the migration of CD4+ T cells and macrophages to the peritoneum.
Targets&IC50
[125I]-CXCL10-CXCR3:1.5 nM (Ki, in CXCR3-CHO cell membranes), [125I]-CXCL11-CXCR3:3.2 nM (Ki, in CXCR3-CHO cell membranes)
In vivo
Methods: DBA/1J mice were treated with NBI-74330 (100 mg/kg) in a collagen-induced arthritis (CIA) model. Arthritis scores and histopathological changes were assessed. Flow cytometry was used to investigate the effects of NBI-74330 on Th1 (IFN-γ, TNF-α, T-bet, STAT4, Notch-3, and RANKL), Th17 (IL-21, IL-17A, STAT3, and RORγt), and Th22 (IL-22) cell expression in splenic CD4 and CXCR3 T cells. RT-PCR was used to assess mRNA levels of IFN-γ, TNF-α, T-bet, RANKL, IL-17A, RORγt, and IL-22 in knee joint tissues. ELISA was used to measure serum protein levels of IFN-γ, TNF-α, and IL-17A. Results: The severity of arthritis scores and histological severity of inflammation were significantly reduced in NBI-74330-treated CIA mice. The percentages of CD4IFN-γ, CD4TNF-α, CD4T-bet, CD4STAT4, CD4Notch-3, CXCR3IFN-γ, CXCR3TNF-α, CXCR3T-bet, CXCR3STAT4, CXCR3Notch-3, CD4RANKL, CD4IL-21, CD4IL-17A, CD4STAT3, CD4RORγt, and CD4IL-22 cells were decreased in NBI-74330-treated CIA mice. In addition, NBI-74330 treatment downregulated the mRNA levels of IFN-γ, TNF-α, T-bet, RANKL, STAT3, IL-17A, RORγt, and IL-22. [1]
SynonymsNBI74330
Chemical Properties
Molecular Weight605.58
FormulaC32H27F4N5O3
Cas No.855527-92-3
Smiles[C@@H](N(CC=1C=CC=NC1)C(CC2=CC(C(F)(F)F)=C(F)C=C2)=O)(C)C=3N(C(=O)C=4C(N3)=NC=CC4)C5=CC=C(OCC)C=C5
Relative Density.no data available
Storage & Solubility Information
Storagekeep away from moisture,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: 80 mg/mL (132.1 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+90% Corn Oil: 3.3 mg/mL (5.45 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
1mg5mg10mg50mg
1 mM1.6513 mL8.2565 mL16.5131 mL82.5655 mL
5 mM0.3303 mL1.6513 mL3.3026 mL16.5131 mL
10 mM0.1651 mL0.8257 mL1.6513 mL8.2565 mL
20 mM0.0826 mL0.4128 mL0.8257 mL4.1283 mL
50 mM0.0330 mL0.1651 mL0.3303 mL1.6513 mL
100 mM0.0165 mL0.0826 mL0.1651 mL0.8257 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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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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
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