SCH 546738

SKU: orb1706650

Description

SCH 546738 is a potent and selective oral CXCR3 antagonist used in research. It has demonstrated efficacy in preclinical models, attenuating autoimmune disease progression and delaying allograft rejection in vivo. This small molecule is a valuable tool for studying chemokine receptor function in immunology and transplantation research.

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 906805-42-3
• MW: 492.45
• Purity: 98.67% (May vary between batches)
• Formula: C₂₃H₃₁Cl₂N₇O
• SMILES: ClC=1C(N2C[C@H](CC)N(CC2)C3CCN(CC4=CC=C(Cl)C=C4)CC3)=NC(N)=C(C(N)=O)N1
• Target: CXCR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.03 mM);DMSO:2 mg/mL (4.06 mM);H2O:< 1 mg/mL (2.03 mM, insoluble or slightly soluble.)

Bioactivity

• Target IC50:
  CXCR3 (human):0.4 nM (Ki)|CXCR3-mediated chemotaxis (human activated T cells):10 nM (IC90)
• 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).
• 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.

Storage & Handling

• 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.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CXCR3, Human CXCR3, SCH546738, SCH-546738, SCH 546738

Compound Identifiers

PubChem CID

11995774