SCH-563705( SCH563705 )

Catalog No. M14573 CAS No. 473728-58-4

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Product Name

SCH-563705
Note

Research use only, not for human use.
Brief Description

A potent, orally bioavailable dual CXCR2/CXCR1 receptor antagonist with IC50 of 1.3 nM and 7.3 nM, respectively.
Description

A potent, orally bioavailable dual CXCR2/CXCR1 receptor antagonist with IC50 of 1.3 nM and 7.3 nM, respectively; demonstrates potent inhibition against both Gro-alpha and IL-8 induced hPMN migration (Chemotaxis: CXCR2 IC50=0.5 nM, CXCR1 IC50=37 nM); dose-dependently decreases paw thickness and clearly reduces inflammation, and bone and cartilage degradation in a mouse model of arthritis.
In Vitro

SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively. SCH 563705 shows 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). SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM).
In Vivo

SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys and dogs. SCH 563705 (50 mg/kg p.o) reduces blood Ly6G+ Ly6C+ neutrophil frequency and unchanged levels of Ly6GLy6Chi monocytes. SCH563705 (3-30 mg/kg p.o) treatment causes a dosedependent elevation in plasma levels of CXCL1.
Synonyms

SCH563705
Pathway

GPCR/G Protein
Target

Chemokine Receptor
Recptor

Chemokine Receptor
Research Area

Inflammation/Immunology
Indication

——

CAS Number

473728-58-4
Formula Weight

425.4776
Molecular Formula

C23H27N3O5
Purity

>98% (HPLC)
Solubility

DMSO: ≥30mg/mL
SMILES

CC(C)C1C=C(OC=1)[C@@H](CC)NC2=C(NC3C(O)=C(C=CC=3)C(=O)N(C)C)C(=O)C2=O
Chemical Name

Benzamide, 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-[4-(1-methylethyl)-2-furanyl]propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-

1. Chao J, et al. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3778-83. 2. Min SH, et al. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6.

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