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PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.

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PKRA83 Chemical Structure

PKRA83 Chemical Structure

CAS No. : 1233926-87-8

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5 mg USD 180 In-stock
10 mg USD 315 In-stock
25 mg USD 665 In-stock
50 mg USD 1180 In-stock
100 mg USD 2100 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of PKRA83:

PKRA83 Related Antibodies

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  • Purity & Documentation

  • References

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Description

PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier[1][2][3].

IC50 & Target

IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1]
In Vitro

PKRA83 (1 µg/mL) effectively reduces PK2-induced microvascular endothelial cell branching in vitro[1].
PKRA83 (2 μM, 24 h) blocks the neuroprotective action of rPK2 in dopaminergic N27 cells (rPK2 protects N27 cell against MPP+-induced dopaminergic neuronal cell death)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PKRA83 Related Antibodies
In Vivo

PKRA83 (20 mg/kg; i.p) shows anti-tumor activity in the context of glioblastoma xenograft tumor models[1].
PKRA83 (15 mg/kg; i.p, daily for 2 weeks) inhibits arthritis in mice with collagen-induced arthritis[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model[1]
Dosage: 20 mg/kg
Administration: i.p, daily
Result: Decreased tumor growth rate and tumor weight.
Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
Animal Model: Collagen-induced arthritis in mice[2]
Dosage: 15 mg/kg
Administration: i.p, daily for 2 weeks
Result: Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation).
Lowered IL-1β and 1 L-6 gene expression levels in the joints.
Molecular Weight

505.02

Formula

C27H34ClFN2O4
CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

ClC1=C2C(OCCCO2)=CC(CN(CC(C)C)C([C@H]3CN(CC3)CC4=CC(OC)=C(C=C4)F)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (49.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9801 mL 9.9006 mL 19.8012 mL
5 mM 0.3960 mL 1.9801 mL 3.9602 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9801 mL 9.9006 mL 19.8012 mL 49.5030 mL
5 mM 0.3960 mL 1.9801 mL 3.9602 mL 9.9006 mL
10 mM 0.1980 mL 0.9901 mL 1.9801 mL 4.9503 mL
15 mM 0.1320 mL 0.6600 mL 1.3201 mL 3.3002 mL
20 mM 0.0990 mL 0.4950 mL 0.9901 mL 2.4751 mL
25 mM 0.0792 mL 0.3960 mL 0.7920 mL 1.9801 mL
30 mM 0.0660 mL 0.3300 mL 0.6600 mL 1.6501 mL
40 mM 0.0495 mL 0.2475 mL 0.4950 mL 1.2376 mL
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PKRA83 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PKRA831233926-87-8PKRA7PKRA 83PKRA-83PKRA 7PKRA-7OthersprokineticinPKR1PKR2anticanceranti-angiogenic activitiesblood-brain barrierarthritisInhibitorinhibitorinhibit

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