PKRA 7

Name: PKRA 7
Brand: Tocris Bioscience
SKU: 6238

Tocris Bioscience, part of Bio-Techne | Catalog # 6238

Citations (1)

COA / SDS

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
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)
Molecular Weight:	541.48

View Full Technical Details for PKRA 7

Technical Data
Citations

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 for PKRA 7

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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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References for PKRA 7

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