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PKRA83 hydrochloride hydrate, also known as PKRA7, is a potent prokineticin (PK2) antagonist that competes with PK2 for binding to its receptors, PKR1 and PKR2. It exhibits high inhibitory affinity with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2, displaying anticancer, anti-arthritis, and anti-angiogenic properties. Additionally, this compound is capable of crossing the blood-brain barrier [1] [2] [3].
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Description | PKRA83 hydrochloride hydrate, also known as PKRA7, is a potent prokineticin (PK2) antagonist that competes with PK2 for binding to its receptors, PKR1 and PKR2. It exhibits high inhibitory affinity with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2, displaying anticancer, anti-arthritis, and anti-angiogenic properties. Additionally, this compound is capable of crossing the blood-brain barrier [1] [2] [3]. |
In vitro | PKRA83 at a concentration of 1 µg/mL effectively reduces microvascular endothelial cell branching induced by PK2 in vitro [1]. |
In vivo | PKRA83 hydrochloride hydrate, administered at a dose of 20 mg/kg via intraperitoneal injection, demonstrated antitumor activity in a xenograft glioblastoma model [1]. Furthermore, when given at 15 mg/kg through intraperitoneal injection daily for two weeks, PKRA83 hydrochloride hydrate inhibited arthritis in mice with collagen-induced arthritis [2]. |
Alias | PKRA7 hydrochloride hydrate |
Storage | Shipping with blue ice. |
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