Dagrocorat

Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat 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 can be used for the research of rheumatoid arthritis[1].

Product Specifications

CAS Number

[1044535-52-5]

Product Name Alternative

PF-00251802

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.html

Purity

99.90

Solubility

DMSO : 250 mg/mL (ultrasonic)

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

Molecular Formula

C29H29F3N2O2

Molecular Weight

494.55

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 Mar;7 (3) :244-255.