PD 168368

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

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

PD 168368 Chemical Structure

CAS No. : 204066-82-0

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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].

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.

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.

分子量

554.64

Formula

C31H34N6O4

CAS 号

204066-82-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [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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