PKRA 7
Tocris Bioscience, part of Bio-Techne | Catalog # 6238
Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
Key Product Details
Description
Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
Alternative Names
PROK2 Antagonist,Bv8 Antagonist,PK2 Antagonist,Prokineticin 2 Antagonist
Product Description
PKRA 7 is a potent prokineticin (PK) receptor antagonist (IC50 values are 5.0 and 8.2 nM for PKR1 and PKR2, respectively). Reduces IL-1β and lL-6 expression in the joints and suppresses severity of arthritis in a mouse model of rheumatoid arthritis. Inhibits PK2-induced expression of pro-migratory chemokines and chemokine receptors in macrophages. Exhibits antitumor activity against glioblastoma and pancreatic cancer xenograft tumor models. Also exhibits antiangiogenic activity in vivo. Brain penetrant. Cell-permeable.Product Specifications
Molecular Weight
541.48
Formula
C27H34ClFN2O4.HCl
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(3R)-N-[(9-Chloro-3,4-dihydro-2H-1,5-benzodioxepin-7-yl)methyl]-1-[(4-fluoro-3-methoxyphenyl)methyl]-N-(2-methylpropyl)-3-pyrrolidinecarboxamide hydrochloride
InChI Key
ICBJJRUEQVVDRU-ZMBIFBSDSA-N
SMILES
FC1=C(OC)C=C(CN2CC[C@H](C2)C(N(CC(C)C)CC3=CC(Cl)=C4OCCCOC4=C3)=O)C=C1.Cl
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.15 | 100 |
Preparing Stock Solutions
for PKRA 7
The following data is based on the product molecular weight 541.48
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.85 mL | 9.23 mL | 18.47 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.69 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.85 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Curtis A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer. PLoS One 2013 PMID: 23372791
- Ito Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis. BMC Musculoskelet.Disord. 2016 PMID: 27609223
Product Specific Notices for PKRA 7
For research use only
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