生物活性

• 描述BX471 is a potent and selective non-peptide CCR1 (CC Chemokine Receptor-1). It competitively displaced the CCR1 ligands MIP-1α, RANTES and MCP-3 with Ki values ranging in 1-5.5nM. BX471 could inhibit a number of CCR1-mediated effects including MIP-1α-induced Ca²⁺ mobilization, increase in extracellular acidification rate, MIP-1α-inducedCD11b expression, and leukocyte and monocyte migration induced by MIP-1α and RANTES. It effectively reduced disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis at doses of 20mg/kg and 50mg/kg^[2].
• 作用机制BX471 can display CCR1 ligands in a competitive manner.^[2]

• 动物研究
  剂量	Mice: 3 mg/kg -30 mg/kg[2] (i.p.); 20 mg/kg[3] (s.c.), 100 mg/kg17234893s (s.c.)
  给药途径	i.p., s.c.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00185341	Endometriosis	Phase 2	Completed	-	Czech Republic ... more >> Hradec Kralove, Czech Republic, 50036 Praha, Czech Republic, 12851 Praha, Czech Republic, 14700 Praha, Czech Republic, 15006 Denmark Aarhus, Denmark, 8200 Glostrup, Denmark, 2600 Finland Helsinki, Finland, 00029 Helsinki, Finland, 00100 Joensuu, Finland, 80210 Kuopio, Finland, 70110 Oulu, Finland, 90100 Turku, Finland, 20100 France Bordeaux, France, 33000 Clermont Ferrand, France, 63000 Lyon, France, 69003 Netherlands Amsterdam, Netherlands, 1061 AE Amsterdam, Netherlands, 1081 HV Maastricht, Netherlands, 6229 HX Nijmegen, Netherlands, 6525 GA Spain Oviedo, Asturias, Spain, 33006 Barcelona, Spain, 08022 Barcelona, Spain, 08036 Madrid, Spain, 28040 Madrid, Spain, 28046 Sevilla, Spain, 41014 Valencia, Spain, 46010 Sweden Göteborg, Sweden, 41685 Lund, Sweden, 22185 Skövde, Sweden, 541 85 Stockholm, Sweden, 141 86 Stockholm, Sweden, 182 88 Uppsala, Sweden, 75185 Collapse <<

• 参考文献

• [1] Liang M, Mallari C, et al. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8.

  [2] Liang M, Mallari C, Rosser M, Ng HP, May K, Monahan S, Bauman JG, Islam I, Ghannam A, Buckman B, Shaw K, Wei GP, Xu W, Zhao Z, Ho E, Shen J, Oanh H, Subramanyam B, Vergona R, Taub D, Dunning L, Harvey S, Snider RM, Hesselgesser J, Morrissey MM, Perez HD. Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem. 2000 Jun 23;275(25):19000-8. doi: 10.1074/jbc.M001222200. PMID: 10748002.