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首页-小分子抑制剂&激动剂-GPCR-Bombesin Receptor-PD168368
PD168368

Chemical Structure : PD168368

CAS No.: 204066-82-0

PD168368 (PD 168368)

货号: PC-21220Not For Human Use, Lab Use Only.

PD168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with Ki of 15 nM, IC50 of 96 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PD168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with Ki of 15 nM, IC50 of 96 nM.
PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50 of 0.57, 0.24, and 2.7 nM, respectively.
PD168368 is highly active and stimulated [Ca2+]I release in human neutrophils with EC50 values in the nanomolar range.
PD168368 suppresses migration and invasion of the human breast cancer cell line MDA-MB-231.
PD168368 reduces epithelial-mesenchymal transition (EMT) of breast cancer cells by E-cadherin upregulation and vimentin downregulation.
PD168368 suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells.
PD168368 potently inhibits in vivo metastasis of breast cancer.

物理化学性质&存储条件

分子量 554.65
分子式 C31H34N6O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-3-(1H-indol-3-yl)-2-methyl-2-(3-(4-nitrophenyl)ureido)-N-((1-(pyridin-2-yl)cyclohexyl)methyl)propanamide

参考文献

1. R R Ryan, et al. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.

2. K Tokita, et al. J Biol Chem. 2001 Jan 5;276(1):495-504.

3. Igor A Schepetkin, et al. Mol Pharmacol. 2011 Jan;79(1):77-90.

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