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SCH 527123

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基本信息:

  • 发布时间: 2017-06-12
  • 产品名称: SCH 527123
  • 产品英文名称: SCH 527123
  • CAS号: 473727-83-2
  • 产品包装: 5 mg
  • 产品价格: 2455元/套
  • 有效期: 一年

产品图片:

SCH 527123

产品描述:

SCH 527123的生物活性

 

SCH-527123 is a potent antagonist of both CXCR1 and CXCR2 with IC50 of 42 nM and 3 nM, respectively.
IC50 value: 42 nM (CXCR1); 3 nM (CXCR2) [1]
Target: CXCR1/2
in vitro: Sch527123 inhibits chemokine binding to CXCR1 and CXCR2 receptors in an insurmountable manner and is categorized as an allosteric antagonist. Sch527123 inhibits neutrophil chemotaxis and myeloperoxidase release in response to CXCL1 and CXCL8 but has no effect on the response of these cells to C5a or formyl-methionyl-leucyl-phenylalanine. Sch527123 binding to CXCR1 and CXCR2 is both saturable and reversible. Sch527123 binds to CXCR1 with good affinity (Kd = 3.9 nM), the compound is CXCR2-selective (Kd = 0.049 nM) [1]. Sch527123 bound with high affinity to the CXCR2 receptors of mouse (Kd = 0.20 nM), rat (Kd = 0.20 nM), and cynomolgus monkey (Kd = 0.08 nM) and is a potent antagonist of CXCR2-mediated chemotaxis (IC50 ~3–6 nM). In contrast, Sch527123 bound to cynomolgus CXCR1 with lesser affinity (Kd = 41 nM) and weakly inhibited cynomolgus CXCR1-mediated chemotaxis (IC50 ~1000 nM) [2].
in vivo: Oral treatment with Sch527123 blocks pulmonary neutrophilia (ED50 = 1.2 mg/kg) and goblet cell hyperplasia (32–38% inhibition at 1–3 mg/kg) in mice following the intranasal lipopolysaccharide (LPS) administration. In rats, Sch527123 suppresses the pulmonary neutrophilia (ED50 = 1.8 mg/kg) and increase in bronchoalveolar lavage (BAL) mucin content (ED50 =<0.1 mg/kg) induced by intratracheal (i.t.) LPS. Sch527123 also suppresses the pulmonary neutrophilia (ED50 = 1.3 mg/kg), goblet cell hyperplasia (ED50 = 0.7 mg/kg), and increase in BAL mucin content (ED50 = <1 mg/kg) in rats after i.t. administration of vanadium pentoxide. In cynomolgus monkeys, Sch527123 reduces the pulmonary neutrophilia induced by repeat bronchoscopy and lavage (ED50 = 0.3 mg/kg) [2].

 

化学信息

分子量
397.42
储存条件
参考CoA中推荐的条件进行储存。
分子式
C21H23N3O5
CAS号
473727-83-2
溶剂/溶解度
Soluble to 100 mM in DMSO

 

相关文献

 

 

[1]. Gonsiorek W, et al. Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist. J Pharmacol Exp Ther. 2007 Aug;322(2):477-85.

[2]. Chapman RW, et al. A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J Pharmacol Exp Ther. 2007 Aug;322(2):486-93.

  • 供应商联系方式:
  • 联系人 谢小姐
  • 公司名称 深圳市浩博世纪生物有限公司
  • 电话 0755-29573896
  • 手机 15994704873
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