产品描述:
ERB 041 is an estrogen receptor β (ERβ) agonist (IC50s = 5.4, 3.1, and 3.7 nM for the human, rat, and mouse receptors, respectively).{53106} It is selective for ERβ over ERα (IC50s = 1,200, 620, and 750 nM for human, rat, and mouse ERα, respectively). ERB 041 induces IGFBP4 mRNA expression in Saos-2 cells expressing human ERβ (EC50 = 20 nM). In vivo, ERB 041 (0.1 and 0.3 mg/kg) inhibits chronic diarrhea and reduces colonic ulceration, inflammation, and fibrosis in the HLA-B27 transgenic rat model of inflammatory bowel disease. It reduces joint swelling in a rat model of adjuvant-induced arthritis when administered at a dose of 1 mg/kg. ERB 041 (10 mg/kg) also reduces lesion formation in a mouse model of endometriosis.{53107}