Mechanism of action: Glucocorticoid Receptor (GR) full agonist
Preclinical pharmacology and pharmacokinetics
AZD2906 is a potent glucocorticoid receptor (2.8 nM) full agonist with selectivity against other steroid nuclear hormone receptors (AR, ER, MR and PR) and an EC50 of 2.2 nM in the human peripheral blood mononuclear cell assay (LPS induced TNF-α production). AZD2906 was demonstrated to be a selective dimerising GR agonist, driving glucocorticoid response element gene expression, and conferred protection in a mouse model of TNF-induced inflammation.
Safety and tolerability
AZD2906 was found to increase the incidence of micronucleated immature erythrocytes (MIE) in the bone marrow of rats given two oral doses at the maximum tolerated level. AZD2906 did not show significant activity in the standard in vitro tests or in vivo in a rat liver comet assay.
Suitable for and exclusions
This compound is offered for preclinical studies only at this time.
Publications for this compound
Find out more about this compound by reading related publications:
Hemmerling, M.; Edman,K.; Lepistö, M.; Eriksson, A.; Ivanova, S.; Dahmen, J.; Rehwinkel, H.; Berger, M.; Hendrickx, R.; Dearman, M.; Jensen, T. J.; Wissler, L.; Hansson, T. Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators. Bioorg. Med. Chem. Lett. 2016, 26, 5741−5748.
Gene information from the NCBi
This compound works on the following genes: