SCH 563705

SKU: orb1706649

Description

SCH 563705 is a potent, orally bioavailable dual antagonist of CXCR2 and CXCR1 chemokine receptors. It is a valuable research tool for investigating neutrophilic inflammation in models of acute respiratory distress syndrome (ARDS) and chronic obstructive pulmonary disease (COPD), both in vitro and in vivo.

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 473728-58-4
• MW: 425.48
• Purity: 98.03% (May vary between batches)
• Formula: C₂₃H₂₇N₃O₅
• SMILES: N(C1=C(N[C@H](CC)C2=CC(C(C)C)=CO2)C(=O)C1=O)C3=C(O)C(C(N(C)C)=O)=CC=C3
• Target: CXCR
• Solubility: DMSO:100 mg/mL (235.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11.75 mM)

Bioactivity

• Target IC50:
  CXCR1:7.3 nM|CXCR1:3 nM (ki)|CXCR2:1.3 nM|CXCR2:1 nM (ki)|CXCR2 (mouse):5.2 nM
• In Vivo:
  SCH 563705 has a favorable oral pharmacokinetic profile in rats, mice, monkeys and dogs. Oral administration of 50 mg/kg SCH 563705 to BALB/c female mice decreased the frequency of Ly6G+ Ly6C+ neutrophils in the blood and maintained the level of Ly6GLy6C hi monocytes.
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• In Vitro:
  SCH 563705 is a potent oral CXCR2 and CXCR1 antagonist with IC50 values of CXCR2 IC50=1.3 nM, CXCR1 IC50=7.3 nM, and Ki values of CXCR2 Ki=1 nM and CXCR1 Ki=3 nM, respectively.SCH 563705 potently inhibits Gro-a and IL-8 induced human neutrophil migration (CXCR2 IC50=0.5 nM, CXCR1 IC50=37 nM). SCH 563705 effectively inhibited Gro-a and IL-8-induced human neutrophil migration (CXCR2 IC50=0.5 nM, CXCR1 IC50=37 nM). SCH 563705 effectively inhibits mouse CXCR2 (IC50 = 5.2 nM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CXCR2, CXCR1, Mouse CXCR2, SCH 563705, SCH-563705

Compound Identifiers

PubChem CID

10310100