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PD 168368
PD 168368 是一种有效的、竞争性的选择性神经调节蛋白 B 受体 (NMB-R) 拮抗剂，Ki 为 15-45 nM。 PD 168368 是神经调节素 B 受体（NMBR; IC50=96 nM）和胃泌素释放肽受体 (GRPR; IC50=3500 nM)）的双重拮抗剂。PD 168368 还是一种 FPR1/FPR2/FPR3 的混合激动剂，EC50 分别为 0.57、0.24 和 2.7 nM。
PD 168368 Chemical Structure
CAS No. : 204066-82-0
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].
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体外研究
(In Vitro) |
PD 168368 (PD168368) is highly active and stimulated [Ca2+]I release in human neutrophils with EC50 values in the nanomolar range[3].
PD 168368 (PD168368) suppresses migration and invasion of the human breast cancer cell line MDA-MB-231. PD 168368 reduces epithelial-mesenchymal transition (EMT) of breast cancer cells by E-cadherin upregulation and vimentin downregulation. PD 168368 (5 μM) inhibits migration and invasiveness in breast cancer cells[4].
PD 168368 (10 μM) suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[4]
| Cell Line: |
Human breast cancer cell line MDA-MB-231 |
| Concentration: |
5 μM |
| Incubation Time: |
24 hours |
| Result: |
Clearly decreased the migratory ability of MDA-MB-231 cells in a Boyden chamber migration assay. |
Cell Viability Assay[4]
| Cell Line: |
MDA-MB-231 cells |
| Concentration: |
10 μM |
| Incubation Time: |
0, 0.5, 1, 2, 4, 8, and 16 hours |
| Result: |
Decreased phosphorylation levels of mTOR, p70S6K, 4EBP1, AKT and GSK-3β in a time-dependent manner. |
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体内研究
(In Vivo) |
PD 168368 (PD168368) potently inhibits in vivo metastasis of breast cancer. PD 168368 (1.2 mg/kg; intraperitoneal injection for 30 days) inhibits metastasis of breast cancer in mice[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Female BALB/c-nude mice (age 8-10 weeks) bearing MDA-MB-231 xenograft model[4] |
| Dosage: |
1.2 mg/kg |
| Administration: |
Intraperitoneal injection for 30 days |
| Result: |
No metastatic tumor nodules were observed in lungs of PD 168368-treated mice compared to PEG-injected mice. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
| Powder |
-20°C |
3 years |
| In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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| 参考文献 |
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[1]. R R Ryan, et al. Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.
[2]. K Tokita, 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. J Biol Chem. 2001 Jan 5;276(1):495-504.
[3]. Igor A Schepetkin, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90.
[4]. Hyun-Joo Park, et al. Neuromedin B receptor antagonism inhibits migration, invasion, and epithelial-mesenchymal transition of breast cancer cells. Int J Oncol. 2016 Sep;49(3):934-42.
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