ERB 041

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).¹ 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.²

WARNING This product is not for human or veterinary use.

1. Harris, H.A., Albert, L.M., Leathurby, Y., et al. Evaluation of an estrogen receptor-β agonist in animal models of human disease. Endocrinology 144(10), 4241-4249 (2003).

2. Harris, H.A., Bruner-Tran, K.L., Zhang, X., et al. A selective estrogen receptor-β agonist causes lesion regression in an experimentally induced model of endometriosis. Hum. Reprod. 20(4), 936-941 (2005).