dagrocorat

InvivoChem Cat #:V4491CAS #:1044535-52-5Purity >=98%

Description: Dagrocorat (also known as PF-00251802) is a novel and potent dissociated glucocorticoid receptor agonist with the potential usefulness as an anti-inflammatory agent. The dissociated agonists of the glucocorticoid receptor are a novel class of agents in clinical development for rheumatoid arthritis. PF-04171327 (fosdagrocorat) is a phosphate ester prodrug of PF-00251802 (dagrocorat), a selective high-affinity partial agonist of the glucocorticoid receptor, which is further metabolized to PF-04015475. PF-00251802 is a reversible inhibitor of several CYPs, but modeling has suggested no clinically relevant interaction. PF-00251802 and PF-04015475 are time-dependent inhibitors and inducers of CYP3A in vitro; PF-00251802 is also a time-dependent inhibitor of CYP2D6. Model-based prediction suggested the potential for weak inhibition of CYP3A in vivo. A clinical DDI study was conducted with midazolam, a sensitive CYP3A substrate. A phase 1 open-label, multiple-dose study evaluated the effect of PF-04171327 on midazolam pharmacokinetics and safety in 12 healthy volunteers. Administration of midazolam alone or concomitantly with PF-04171327 resulted in equivalent pharmacokinetic profiles (AUCinf , 21.17 vs 20.28 ng·h/mL, respectively), indicating that PF-04171327 had no net effect on CYP3A activity in vivo. These findings support the further development of PF-00251802 and PF-04171327 as potential treatments for patients with rheumatoid arthritis (NCT00987038).

References: Clin Pharmacol Drug Dev. 2018 Mar; 7(3):244-255.

Related CAS: 1044535-58-1 (Fosdagrocorat)

-20C for 3 years in powder form

Synonym: PF-251802; PF 251802; PF251802; PF-00251802; PF 00251802; PF00251802;
IUPAC/Chemical Name: (4bR, 7S, 8aR)-4b-benzyl-7-hydroxy-N-(2-methylpyridin-3-yl)-7-(trifluoromethyl)-4b, 5, 6, 7, 8, 8a, 9, 10-octahydrophenanthrene-2-carboxamide
InChi Key: QJJBNCHSWFGXML-QPVYNBJUSA-N
InChi Code: InChI=1S/C29H29F3N2O2/c1-19-25(8-5-15-33-19)34-26(35)22-10-12-24-21(16-22)9-11-23-18-28(36, 29(30, 31)32)14-13-27(23, 24)17-20-6-3-2-4-7-20/h2-8, 10, 12, 15-16, 23, 36H, 9, 11, 13-14, 17-18H2, 1H3, (H, 34, 35)/t23-, 27-, 28+/m1/s1
SMILES Code: FC([C]1(O)CC[C]2(CC3=CC=CC=C3)C4=CC=C(C(NC5=CC=CN=C5C)=O)C=C4CC[C]2([H])C1)(F)F