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SCH 563705

Catalog No. T16864   CAS 473728-58-4

SCH 563705 is an effective and orally available CXCR2 and CXCR1 antagonist (IC50s: 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively).

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SCH 563705 Chemical Structure
SCH 563705, CAS 473728-58-4
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 2,270.00
50 mg 10-14 weeks $ 2,980.00
100 mg 10-14 weeks $ 4,000.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SCH 563705 is an effective and orally available CXCR2 and CXCR1 antagonist (IC50s: 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively).
Targets&IC50 Mouse CXCR2:5.2 nM, CXCR1:3 nM (ki), CXCR1:7.3 nM, CXCR2:1 nM (ki), CXCR2:1.3 nM
In vitro SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM). SCH 563705 displays potent inhibition against both Gro-a and IL-8 induced human neutrophil migration (chemotaxis IC50 = 0.5 nM, against 30 nM of Gro-a; chemotaxis IC50 = 37 nM, against 3 nM of IL-8) [1][2].
In vivo SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys, and dogs. SCH563705 (3-30 mg/kg p.o) treatment causes a dose-dependent elevation in plasma levels of CXCL1. SCH 563705 (50 mg/kg p.o) decreases blood Ly6G+ Ly6C+ neutrophil frequency and unchanged levels of Ly6GLy6Chi monocytes [1][2].
Molecular Weight 425.48
Formula C23H27N3O5
CAS No. 473728-58-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (70.51 mM)

TargetMolReferences and Literature

1. Chao J, et al. C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3778-83. 2. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6.

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Keywords

SCH 563705 473728-58-4 Autophagy GPCR/G Protein Immunology/Inflammation CXCR SCH-563705 SCH563705 inhibitor inhibit

 

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