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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $199 | - | In Stock |
| 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] |
| Synonyms | SCH546738 |
| Molecular Weight | 492.45 |
| Formula | C23H31Cl2N7O |
| Cas No. | 906805-42-3 |
| Smiles | ClC=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 | 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: 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
| |||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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