PKRA 7

Catalog # Availability Size / Price Qty
6238/5
PKRA 7 | Prokineticin R2/PROKR2
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Description: Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
Alternative Names: PROK2 Antagonist, Bv8 Antagonist, PK2 Antagonist, Prokineticin 2 Antagonist

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

Purity: ≥98%

Product Details
Reviews

Biological Activity

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.

Technical Data

M.Wt:
541.48
Formula:
C27H34ClFN2O4.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C

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.

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