PKRA 7

Pricing Availability   Qty
说明: Potent prokineticin (PK) 1 and 2 receptor antagonist; antitumor; BBB penetrant
别名: PROK2 Antagonist,Bv8 Antagonist,PK2 Antagonist,Prokineticin 2 Antagonist
化学名: (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
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (1)

生物活性 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.

技术数据 for PKRA 7

分子量 541.48
公式 C27H34ClFN2O4.HCl
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PKRA 7

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 54.15 100

制备储备液 for PKRA 7

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for PKRA 7

参考文献是支持产品生物活性的出版物。

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


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