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].

Product Specifications

CAS Number

[1044535-61-6]

Product Name Alternative

PF-00251802 (hydrochloride)

UNSPSC

12352005

Target

Cytochrome P450; Glucocorticoid Receptor

Type

Reference compound

Related Pathways

Immunology/Inflammation; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Endocrinology; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/dagrocorat-hydrochloride.html

Purity

99.85

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O[C@@]1(C(F)(F)F)C[C@]2([H])[C@](C3=CC=C(C(NC(C=CC=N4)=C4C)=O)C=C3CC2)(CC1)CC5=CC=CC=C5.[H]Cl

Molecular Formula

C29H30ClF3N2O2

Molecular Weight

531.01

References & Citations

[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.