[CAS NO. 473728-58-4] SCH 563705
PRODUCTS SPECIFICATIONS [473728-58-4]
DESCRIPTION [473728-58-4]
Overview
| MDL | MFCD11035877 |
|---|---|
| Molecular Weight | 425.48 |
| Molecular Formula | C23H27N3O5 |
| SMILES | O=C(C(NC1=CC=CC(C(N(C)C)=O)=C1O)=C2N[C@H](CC)C3=CC(C(C)C)=CO3)C2=O |
3 Publications Citing Use of MCE
Summary
IC50 & Target
|
CXCR2 1 nM (Ki) |
CXCR1 3 nM (Ki) |
CXCR2 1.3 nM (IC 50 ) |
CXCR1 7.3 nM (IC 50 ) |
Mouse CXCR2 5.2 nM (IC 50 ) |
In Vitro
SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC 50 s of 1.3 nM, 7.3 nM and K i s of 1 and 3 nM, respectively. SCH 563705 shows potent inhibition against both Gro-a and IL-8 induced human neutrophil migration (chemotaxis IC 50 = 0.5 nM, against 30 nM of Gro-a; chemotaxis IC 50 = 37 nM, against 3 nM of IL-8) [1] . SCH 563705 potently inhibits mouse CXCR2 (IC 50 = 5.2 nM) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 30 mg/mL ( 70.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3503 mL | 11.7514 mL | 23.5029 mL |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3503 mL |
References
- [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.
