PD 168368 |
| Catalog No.GC44584 |
PD 168368은 15-45nM의 Ki를 갖는 강력하고 경쟁적이며 선택적인 뉴로메딘 B 수용체(NMB-R) 길항제입니다. PD 168368은 뉴로메딘 B 수용체(NMBR; IC50=96 nM)/가스트린-방출 펩티드 수용체(GRPR IC50=3500 nM) 길항제입니다. PD 168368은 또한 각각 0.57, 0.24 및 2.7nM의 EC50을 갖는 혼합 FPR1/FPR2/FPR3 작용제입니다.
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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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