SCH-563705

Research use only, not for human use.

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

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.

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).

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.

SCH563705

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Inflammation/Immunology

——

473728-58-4

425.4776

C23H27N3O5

>98% (HPLC)

DMSO: ≥30mg/mL

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

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]-

(-20℃)

With Ice Pack

≥ 2 years