Dagrocorat hydrochloride

Names

[ Name ]:
Dagrocorat hydrochloride

[Synonym ]:
unii-vl45kv749o

Biological Activity

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₀ClF₃N₂O₂

[ Molecular Weight ]:
531.01

[ Exact Mass ]:
530.19500

[ PSA ]:
62.22000

[ LogP ]:
7.03750

Related Compounds

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