SMILES string
N([C@H](CC)c3[o]c(cc3)C)c1[c]([c](c1Nc2c(c(ccc2)C(=O)N(C)C)O)=O)=O
InChI key
RXIUEIPPLAFSDF-CYBMUJFWSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Orally active, high-affinity, potent and selective allosteric CXCR2 antagonist.
SCH-527123 is an orally active, high-affinity, potent and selective allosteric CXCR2 antagonist (IC50 = 2.6 nM) with much reduced CXCR1 potency (IC50 = 36 nM) and little activity against a large panel of enzymes, channels, and GPCRs (IC50 >10 µM). SCH-527123 blocks CXCL8- and CXCL1-induced human neutrophil (hPMN) chemotaxis in cultures (IC50 = 16 & <1 nM, respectively) and pulmonary neutrophilia in vivo (ED50 = 1.2 mg/kg mouse, 1.8 mg/kg rat p.o.) following intranasal LPS administration.
SCH-527123 is an orally active, high-affinity, potent and selective allosteric CXCR2 antagonist (IC50 = 2.6 nM) with much reduced CXCR1 potency (IC50 = 36 nM) and little activity against a large panel of enzymes, channels, and GPCRs (IC50 >10 µM). SCH-527123 blocks CXCL8- and CXCL1-induced human neutrophil (hPMN) chemotaxis in cultures (IC50 = 16 & <1 nM, respectively) and pulmonary neutrophilia in vivo (ED50 = 1.2 mg/kg mouse, 1.8 mg/kg rat p.o.) following intranasal LPS administration.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Waldemar Gonsiorek et al.
The Journal of pharmacology and experimental therapeutics, 322(2), 477-485 (2007-05-15)
In neutrophils, growth-related protein-alpha (CXCL1) and interleukin-8 (CXCL8), are potent chemoattractants (Cytokine 14:27-36, 2001; Biochemistry 42:2874-2886, 2003) and can stimulate myeloperoxidase release via activation of the G protein-coupled receptors CXCR1 and CXCR2. The role of CXCR1 and CXCR2 in the
Michael P Dwyer et al.
Journal of medicinal chemistry, 49(26), 7603-7606 (2006-12-22)
Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent
Richard W Chapman et al.
The Journal of pharmacology and experimental therapeutics, 322(2), 486-493 (2007-05-15)
Sch527123 [2-hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]ben-zamide] is a potent, selective antagonist of the human CXCR1 and CXCR2 receptors (Gonsiorek et al., 2007). Here we describe its pharmacologic properties at rodent CXCR2 and at the CXCR1 and CXCR2 receptors in the cynomolgus monkey, as well
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