| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 1.3 μM (CYP3A in human liver microsomes); IC50: 0.57 μM (CYP2D6 in human liver microsomes) | ||||||||||||
| Invitro | Dagrocorat is metabolized by cytochrome P450 (CYP)3A to an N-oxide metabolite. Dagrocorat is a reversible inhibitor of several CYPs, such as CYP3A and CYP2D6[1]. | ||||||||||||
| Name | Dagrocorat | ||||||||||||
| CAS | 1044535-52-5 | ||||||||||||
| Formula | C29H29F3N2O2 | ||||||||||||
| Molar Mass | 494.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Dagrocorat
CAS: 1044535-52-5 F: C29H29F3N2O2 W: 494.55
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor.
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