Dagrocorat hydrochloride

Modify Date: 2024-01-08 02:10:20

Dagrocorat hydrochloride Structure
Dagrocorat hydrochloride structure
Common Name Dagrocorat hydrochloride
CAS Number 1044535-61-6 Molecular Weight 531.01
Density N/A Boiling Point N/A
Molecular Formula C29H30ClF3N2O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Dagrocorat hydrochloride


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].

 Names

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
Synonym More Synonyms

 Dagrocorat hydrochloride 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
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

 Synonyms

unii-vl45kv749o
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