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SCH 546738

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Catalog No. T16863Cas No. 906805-42-3
Alias SCH546738

SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.

SCH 546738

SCH 546738

😃Good
Purity: 98.67%
Catalog No. T16863Alias SCH546738Cas No. 906805-42-3
SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.
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2 mg$199-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:98.67%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
SCH 546738 is an orally available, selective and potent CXCR3 antagonist that attenuates the development of autoimmune diseases and delays graft rejection.
Targets&IC50
CXCR3-mediated chemotaxis (human activated T cells):10 nM (IC90), CXCR3 (human):0.4 nM (Ki)
In vitro
SCH 546738 effectively and specifically inhibits CXCR3-mediated chemotaxis in human activated T cells (IC90=10 nM). SCH 546738 displaces radiolabeled CXCL10 and CXCL11 from human CXCR3 (IC50: ranging from 0.8 to 2.2 nM) in a non-competitive manner. Competition of human CXCL10 and CXCL11 binding to human CXCR3 by SCH 546738 is determined at various concentrations of [125I]hCXCL10 and [125I]hCXCL11 around the Kd (50-100 pM) for the receptor. [1]
In vivo
SCH 546738 is a selective and effective CXCR3 antagonist with a good PK for in vivo studies. SCH 546738 has a favorable pharmacokinetic profile in rodents, the plasma concentrations of SCH 546738 in Lewis rat, and C57BL/6 mouse over 24 hr post-dose. SCH 546738 has strong cross-species activities in inhibiting the binding of [125I]hCXCL10 to CXCR3 of monkey (IC50 = 1.3 nM), dog (IC50 = 6.4 nM), mouse (IC50 = 5.9 nM) and rat origin (IC50 = 4.2 nM). [1]
SynonymsSCH546738
Chemical Properties
Molecular Weight492.45
FormulaC23H31Cl2N7O
Cas No.906805-42-3
SmilesClC=1C(N2C[C@H](CC)N(CC2)C3CCN(CC4=CC=C(Cl)C=C4)CC3)=NC(N)=C(C(N)=O)N1
Relative Density.1.326 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore 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: 2 mg/mL (4.06 mM), Sonication is recommended.
H2O: < 1 mg/mL (2.03 mM, insoluble or slightly soluble.)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.03 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
H2O/DMSO
1mg5mg10mg50mg
1 mM2.0307 mL10.1533 mL20.3066 mL101.5332 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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%
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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

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