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Submit ReviewPKRA 7
Description: Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
Alternative Names: PROK2 Antagonist,Bv8 Antagonist,PK2 Antagonist,Prokineticin 2 Antagonist
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
Purity: ≥98% (HPLC)
Biological Activity for PKRA 7
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.
Technical Data for PKRA 7
| M. Wt | 541.48 |
| Formula | C27H34ClFN2O4.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PKRA 7
| 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 will 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 |
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Product Datasheets for PKRA 7
References for PKRA 7
References are publications that support the biological activity of the product.
Ito et al (2016) Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis. BMC Musculoskelet.Disord. 17 387 PMID: 27609223
Curtis et al (2013) A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer. PLoS One 8 e54916 PMID: 23372791
If you know of a relevant reference for PKRA 7, please let us know.
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Citations for PKRA 7
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Peptides Involved in Appetite Modulation Scientific Review
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