中文名 | (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE |
英文名 | (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE |
别名 | 化合物 T16449 (2S)-3-(1H-吲哚-3-基)-N-[1-(5-甲氧基吡啶-2-基)环己基]-2-甲基-2-[(4-硝基苯基)氨基甲酰氨基]丙酰胺 |
英文别名 | PD 176252 (2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE (S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide 1H-Indole-3-propanamide, N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-, (αS)- |
CAS | 204067-01-6 |
化学式 | C32H36N6O5 |
分子量 | 584.67 |
密度 | 1.297±0.06 g/cm3(Predicted) |
沸点 | 838.8±65.0 °C(Predicted) |
酸度系数 | 11.60±0.46(Predicted) |
存储条件 | Store at +4°C |
体外研究 | PD176252 is a potent antagonist of neuromedin-B preferring (BB 1 ) and gastrin-releasing peptide-preferring (BB 2 ) receptor with K i s of 0.17 nM and 1 nM for human BB 1 and BB 2 receptors, and 0.66 nM, 16 nM for Rat BB 1 and BB 2 receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB 1 or BB 2 receptors expressed in CHO cells, with the appK B s of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB 1 or BB 2 receptors, with appK B s of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC 50 s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca 2+ mobilization in HL-60 cells transfected with human FPRs (EC 50 , 0.72 ± 0.21 μM). PD176252 inhibits little specific 125 I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC 50 of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC 50 s of 7 and 5 μM. |
体内研究 | PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice. |
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