For research use only. Not for therapeutic Use.
SCH 563705 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 (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)[1]. SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM)[2].
SCH 563705 has good oral pharmacokinetic profiles in rats, mice, monkeys and dogs[1]. 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[2].
| Catalog Number | I003642 |
| CAS Number | 473728-58-4 |
| Synonyms | 3-[[3,4-dioxo-2-[[(1R)-1-(4-propan-2-ylfuran-2-yl)propyl]amino]cyclobuten-1-yl]amino]-2-hydroxy-N,N-dimethylbenzamide |
| Molecular Formula | C23H27N3O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H27N3O5/c1-6-15(17-10-13(11-31-17)12(2)3)24-18-19(22(29)21(18)28)25-16-9-7-8-14(20(16)27)23(30)26(4)5/h7-12,15,24-25,27H,6H2,1-5H3/t15-/m1/s1 |
| InChIKey | DGKQQEVYYPCMNE-OAHLLOKOSA-N |
| SMILES | CCC(C1=CC(=CO1)C(C)C)NC2=C(C(=O)C2=O)NC3=CC=CC(=C3O)C(=O)N(C)C |
| Reference | [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. |
