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 ActivityPKRA 7 is a potent 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.
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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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