PD 168368 |
| カタログ番号GC44584 |
PD 168368 は、15 ～ 45 nM の Ki を持つ、強力で競合的かつ選択的なニューロメジン B 受容体 (NMB-R) 拮抗薬です。 PD 168368 はニューロメジン B 受容体 (NMBR; IC50=96 nM) / ガストリン放出ペプチド受容体 (GRPR IC50=3500 nM) 拮抗薬です。 PD 168368 は、それぞれ 0.57、0.24、および 2.7 nM の EC50 を持つ混合 FPR1/FPR2/FPR3 アゴニストでもあります。
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Cas No.: 204066-82-0
Sample solution is provided at 25 µL, 10mM.
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PD 168368 is a competitive antagonist of neuromedin B (NMB) receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines). It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors. PD 168368 is selective for NMB receptors over those for related peptide agonists, including bombesin and gastrin-releasing peptide. It is also an agonist of formyl-peptide receptors (FPRs) at higher concentrations (EC50s = 0.57 and 0.24 µM for FPR1 and FPR2, respectively). PD 168368 induces cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells and blocks neovascularization and cancer cell growth in breast cancer xenograft tumors in mice.
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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