Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
PKRA 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.
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-126337 |
| Réf. fabricant | 18776216 |
| Nom chimique ou matériau | (3 R)-N-[(9-Chloro-3,4-dihydro-2 H-1,5-benzodioxepin-7-yl)methyl]-1-[(4-fluoro-3-methoxyphenyl)methyl]-N-(2-methylpropyl)-3-pyrrolidinecarboxamide hydrochloride |
| Quantité | 5 mg |
| Cible | Prokineticin R2/PROKR2 |
| Formule moléculaire | C<sub>27</sub>H<sub>34</sub>ClFN<sub>2</sub>O<sub>4</sub>.HCl |
| Pureté | 0.98 |
