(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE
- CAS号:204067-01-6
- 英文名:(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
- 中文名:(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE
- CBNumber:CB02453426
- 分子式:C32H36N6O5
- 分子量:584.67
- MOL File:204067-01-6.mol
- 沸点 :838.8±65.0 °C(Predicted)
- 密度 :1.297±0.06 g/cm3(Predicted)
- 储存条件 :Store at +4°C
- 溶解度 :Soluble to 100 mM in DMSO
- 形态 :Powder
- 酸度系数(pKa) :11.60±0.46(Predicted)
- 颜色 :Light yellow to yellow
(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE性质、用途与生产工艺
- 生物活性 PD176252 是一种有效的 BB1 和 BB2 拮抗剂,能够抑制人 BB1 和 BB2 受体和大鼠 BB1 和 BB2 受体活性,Ki 值分别为 0.17 nM,1 nM 和 0.66 nM,16 nM;PD176252 同时为 FPR1/FPR2 的激动剂,在 HL-60 细胞中,EC50 值分别为 0.31 和 0.66 μM。
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靶点
Ki: 0.17 nM (Human BB 1 receptor), 0.66 nM (Rat BB 1 receptor), 1 nM (Human BB 2 receptor), 16 nM (Rat BB 2 receptor)
EC50: 0.31 μM (FPR1), 0.66 μM (FPR2) -
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.
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体内研究
PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice.
- 更新日期:2024/08/19
- 产品编号:HY-103286
- 产品名称:(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE PD176252
- CAS编号:204067-01-6
- 包装:5mg
- 价格:700元
- 更新日期:2024/08/19
- 产品编号:HY-103286
- 产品名称:(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE PD176252
- CAS编号:204067-01-6
- 包装:10mM * 1mLin DMSO
- 价格:900元
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