PD 168368 是一种有效、竞争性和选择性的神经调节蛋白 B 受体 (NMB-R) 拮抗剂，Ki 为 15-45 nM。 PD 168368 是神经调节蛋白 B 受体 (NMBR; IC50=96 nM) / 胃泌素释放肽受体 (GRPR IC50=3500 nM) 拮抗剂。 PD 168368 还是一种混合 FPR1/FPR2/FPR3 激动剂，EC50 分别为 0.57、0.24 和 2.7 nM。
| Cas No. | 204066-82-0 |
| Canonical SMILES | O=C(NCC1(CCCCC1)C2=CC=CC=N2)[C@@](C)(NC(NC3=CC=C(C=C3)[N+]([O-])=O)=O)CC4=CNC5=C4C=CC=C5 |
| 分子式 | C31H34N6O4 |
| 分子量 | 554.6 |
| 溶解度 | DMF: 10 mg/mL,DMSO: 30 mg/mL,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/mL |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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). 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. |
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