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Submit ReviewPKRA 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.
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 54.15 | 100 |
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.
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 |
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
If you know of a relevant reference for PKRA 7, please let us know.
关键词: PKRA 7, PKRA 7 supplier, 1233926-87-8, PKRA7, PKRA_7, potent, prokineticin2, PROK2, PK2, Bv8, PROKR1, PKR1, PKR2, antagonists, antagonises, antagonizes, antagonism, brain, penetrant, Antagonist, Prokineticin, 2, Other, Peptide, Receptors, 6238, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.