PKRA 7

Tocris Bioscience | Catalog # 6238

Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
Tocris Bioscience
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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 for PKRA 7

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.

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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.

Select a batch to recalculate based on the batch molecular weight:

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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Background References

References are publications that support the biological activity of the product.

Product Documents for PKRA 7

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for PKRA 7

For research use only

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