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(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE

(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE, 204067-01-6, 结构式
(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
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)-
中文名:
(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE
中文别名:
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
CBNumber:
CB02453426
分子式:
C32H36N6O5
分子量:
584.67
MOL File:
204067-01-6.mol

(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE化学性质

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
安全信息

(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。

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.

体内研究

PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice.

(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE 上下游产品信息

上游原料

下游产品

(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE 试剂级价格

更新日期产品编号产品名称CAS编号包装价格
2024/04/30HY-103286(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE
PD176252
204067-01-65mg700元
2024/04/30HY-103286(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE
PD176252
204067-01-610mM * 1mLin DMSO900元

(2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE 生产厂家

供应商联系电话电子邮件国家产品数优势度
武汉易泰科技有限公司上海分公司 821-50328103-801 18930552037 3bsc@sina.com 中国 15848 69
EMMX Biotechnology LLC 888-539-0666 info@emmx.com 美国 8449 60
济南药研药物化学有限公司 jnyaoyan@163.com 中国 3069 58
南京美韬医药科技有限公司 meitaochem@126.com meitaochem@126.com 中国 19105 58
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美国 19892 58
BOC Sciences info@bocsci.com 美国 0 65
天津普西唐生物医药科技有限公司 010-60605840 psaitong@jm-bio.com 中国 29778 58
金瓯生物医药(南京)有限公司 13000000000 jinoupharma@163.com 中国 11732 58
开封明仁药业有限公司 0371-65741762 sales@hasunny.com 中国 2380 58
南通全益生物科技有限公司 0513-66337626 18051384581 sales@chemhifuture.com 中国 4370 58
Aladdin Scientific +1-+1(833)-552-7181 sales@aladdinsci.com 美国 52927 58
ApexBio技术 sales@apexbt.com 美国 6254 58
 

204067-01-6, (2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE 相关搜索:

  • C32H36N6O5
  • 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
  • 204067-01-6
  • 1H-Indole-3-propanamide, N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-, (αS)-
  • (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]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide
  • PD 176252
  • (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
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