PKRA83
Based on 1 Customer Validation
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. .
For research use only. We do not sell to patients.
- Purity: 98.95%
- CAS No.: 1233926-87-8
- Formula: C27H34ClFN2O4
- Molecular Weight:505.02
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Storage:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1]
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 (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.
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Animal Model:glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model[1]
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Dosage:20 mg/kg
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Administration:i.p, daily
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Result:Decreased tumor growth rate and tumor weight.
Decreased relative blood vessel density and Increased areas of necrotic regions in tumors.
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Animal Model:Collagen-induced arthritis in mice[2]
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Dosage:15 mg/kg
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Administration:i.p, daily for 2 weeks
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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.
Chemical Information
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CAS No. 1233926-87-8
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Appearance Oil
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Molecular Weight 505.02
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Formula C27H34ClFN2O4
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Color Colorless to light yellow
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SMILES
ClC1=C2C(OCCCO2)=CC(CN(CC(C)C)C([C@H]3CN(CC3)CC4=CC(OC)=C(C=C4)F)=O)=C1
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Synonyms
PKRA7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Valerie F Curtis, et al. A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer. PLoS One. 2013;8(1):e54916. [Content Brief]
[2]. Ito H, et al. Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis. BMC Musculoskelet Disord. 2016 Sep 8;17(1):387. [Content Brief]
[3]. Gordon R, et al. Prokineticin-2 upregulation during neuronal injury mediates a compensatory protective response against dopaminergic neuronal degeneration. Nat Commun. 2016 Oct 5;7:12932. [Content Brief]
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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