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PKRA83 hydrochloride

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Catalog No. T212408
Alias PKRA7 hydrochloride

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.

PKRA83 hydrochloride

PKRA83 hydrochloride

😃Good
Catalog No. T212408Alias PKRA7 hydrochloride
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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Product Introduction

Bioactivity
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.
SynonymsPKRA7 hydrochloride
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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