PD 168368
Cat. No.:YN322383
产品名称: | PD 168368 |
CAS No.: | 204066-82-0 |
Chemical Name: | (αS)-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-N-[[1-(2-pyridinyl)cyclohexyl]methyl]-1H-indole-3-propanamide |
Synonyms: | PD 168368; PD168368; PD-168368. |
分子量: | 554.6 |
分子式: | C31H34N6O4 |
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 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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。 |
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Ryan, R.R., Katsuno, T., Mantey, S.A., et al.Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368J. Pharmacol. Exp. Ther.290(3),1202-1211(1999)
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 PD168368J. Biol. Chem.276(1),495-504(2016)
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 receptorsMol. Pharmacol.79(1),77-90(2011)
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 vivoCancer Lett.312(1),117-127(2011)