1044535-61-6

1044535-61-6 structure

Name: Dagrocorat hydrochloride
Chemical Name: (4bS,7R,8aR)-4b-benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-5,6,8,8a,9,10-hexahydrophenanthrene-2-carboxamide,hydrochloride
CAS Number: 1044535-61-6
Molecular Formula: C₂₉H₃₀ClF₃N₂O₂
Molecular Weight: 531.01
Catalog: Signaling Pathways GPCR/G Protein Glucocorticoid Receptor
Create Date: 2017-09-22 20:03:31
Modify Date: 2024-01-08 02:10:20
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis[1].

Name	(4bS,7R,8aR)-4b-benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-5,6,8,8a,9,10-hexahydrophenanthrene-2-carboxamide,hydrochloride
Synonyms	unii-vl45kv749o

Description	Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis[1].
Related Catalog	Research Areas >> Endocrinology Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450 Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor
Target	CYP3A CYP2D6
In Vitro	Dagrocorat hydrochloride is metabolized by cytochrome P450 (CYP)3A to an N-oxide metabolite. Dagrocorat hydrochloride is a reversible inhibitor of several CYPs, such as CYP3A and CYP2D6[1].
References	[1]. Ripp SL, et al. In Vitro and In Vivo Investigation of Potential for Complex CYP3A Interaction for PF-00251802 (Dagrocorat), a Novel Dissociated Agonist of the Glucocorticoid Receptor. Clin Pharmacol Drug Dev. 2018;7(3):244-255.