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PKRA83 (PKRA7) hydrochloride is a potent prokinetic (PK2) antagonist capable of crossing the blood-brain barrier, competitively inhibiting PK2 from binding to its receptors PKR1 and PKR2. It effectively suppresses PK2 receptors, with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2, and exhibits anticancer, anti-arthritis, and anti-angiogenic activities.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | PKRA83 (PKRA7) hydrochloride is a potent prokinetic (PK2) antagonist capable of crossing the blood-brain barrier, competitively inhibiting PK2 from binding to its receptors PKR1 and PKR2. It effectively suppresses PK2 receptors, with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2, and exhibits anticancer, anti-arthritis, and anti-angiogenic activities. |
| In vitro | PKRA83 (1 µg/mL) hydrochloride effectively reduces microvascular endothelial cell branching induced by PK2 in vitro. Additionally, PKRA83 (2 μM, 24 hours) hydrochloride inhibits the neuroprotective effect of rPK2 in dopaminergic N27 cells, preventing rPK2 from safeguarding N27 cells against MPP+-induced dopaminergic neuronal cell death. |
| In vivo | PKRA83 (20 mg/kg; IP) hydrochloride exhibits antitumor activity in a glioblastoma xenograft tumor model. Additionally, PKRA83 (15 mg/kg; intraperitoneal injection, administered once daily for two weeks) hydrochloride is effective in suppressing arthritis in mice with collagen-induced arthritis. |
| Synonyms | PKRA7 hydrochloride |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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