| 货号 | 17920-500ug |
| 描述 | 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).1,2 It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.1 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).3 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.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ryan, R.R.,Katsuno, T.,Mantey, S.A., et al. Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. Journal of Pharmacology and Experimental Therapeutics 290(3), 1202-1211 (1999). 2.Tokita, K.,Hocart, S.J.,Katsuno, T., et al. Tyrosine 220 in the 5th transmembrane domain of the neuromedin B receptor is critical for the high selectivity of the peptoid antagonist PD168368. The Journal of Biological Chemisty 276(1), 495-504 (2016). 3.Schepetkin, I.A.,Kirpotina, L.N.,Khlebnikov, A.I., et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Molecular Pharmacology 79(1), 77-90 (2011). 4.Park, H.J.,Kim, S.R.,Kim, M.K., et al. Neuromedin B receptor antagonist suppresses tumor angiogenesis and tumor growth in vitro and in vivo. Cancer Letters 312(1), 117-127 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 554.6 |
| 分子式 | C31H34N6O4 |
| CAS号 | 204066-82-0 |
| 稳定性 | ≥ 2 years |
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