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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 | Availability | Quantity |
---|---|---|---|
2 mg | $236 | 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 in human activated T cells:10 nM (IC90) |
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] |
Alias | 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. | ||||||||||
Solubility Information | DMSO: 2 mg/mL, (4.06 mM.), Sonication is recommended. H2O: < 1 mg/mL (2.03 mM, insoluble or slightly soluble.) | ||||||||||
Solution Preparation Table | |||||||||||
H2O/DMSO
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