Chemical Name: (3R)-N-[(9-Chloro-3,4-dihydro-2H-1,5-benzodioxepin-7-yl)methyl]-1-[(4-fluoro-3-methoxyphenyl)methyl]-N-(2-methylpropyl)-3-pyrrolidinecarboxamide hydrochloride
Biological ActivityPotent prokineticin (PK) receptor antagonist (IC50 values are 5.0 and 8.2 nM for PKR1 and PKR2, respectively). Reduces IL-1β and lL-6 expression in the joints and suppresses severity of arthritis in a mouse model of rheumatoid arthritis. Inhibits PK2-induced expression of pro-migratory chemokines and chemokine receptors in macrophages. Exhibits antitumor activity against glioblastoma and pancreatic cancer xenograft tumor models. Also exhibits antiangiogenic activity in vivo. Brain penetrant. Cell-permeable.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis.
Ito et al.
BMC Musculoskelet.Disord., 2016;17:387
A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer.
Curtis et al.
PLoS One, 2013;8:e54916
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