1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼

概述生物活性靶點體外研究體內(nèi)研究 用途與合成方法 MSDS 1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼價格(試劑級) 上下游產(chǎn)品信息 專題

中文名稱	1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼
中文同義詞	1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼;男用口服避孕藥;ADJUDIN,通道阻斷劑;1-(2,4-二氯芐基)-1H-吲唑-3-甲酰肼
英文名稱	Adjudin
英文同義詞	1-(2,4-dichlorobenzyl)indazole-3-carbohydrazide;CS-2018;AF-2364;1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide;Adjudin, AF-2364;Adjudin;1-[(2,4-Dichlorophenyl)methyl]-1H-indazole-3-carboxylic acid hydrazide;1-(2,4-Dichloro-benzyl)-1H-indazole-3-carboxylic acid hydrazide
CAS號	252025-52-8
分子式	C15H12Cl2N4O
分子量	335.19
EINECS號
相關(guān)類別	小分子抑制劑;小分子抑制劑，天然產(chǎn)物;定制中心;Inhibitors;pharmaceutical intermedaite
Mol文件	252025-52-8.mol
結(jié)構(gòu)式

1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼 性質(zhì)

1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼 用途與合成方法

概述

Adjudin【男用口服避孕藥（1-(2，4-二氯芐基)-1H-吲唑-3-碳酰肼）】系Lonidamine衍生物。以往在大鼠、家兔及獵犬研究證明Adjudin【男用口服避孕藥（1-(2，4-二氯芐基)-1H-吲唑-3-碳酰肼）】是以種潛在的男性口服避孕藥，它通過干擾睪丸支持細胞和生精細胞的粘附連接，由此引起成熟前生精上皮精子細胞釋放，導致雄性不育。然而，Adjudin【男用口服避孕藥（1-(2，4-二氯芐基)-1H-吲唑-3-碳酰肼）】是否干擾人精子的受精能力及其可能的作用機制，至今尚未研究。

生物活性

Adjudin (AF-2364) 是一種有效的男性避孕藥，也是一種有效的 Cl? channels 的阻滯劑。Adjudin 通過抑制 NF-κB p65核易位和DNA結(jié)合活性以及 ERK MAPK磷酸化而具有抗炎特性。

靶點

體外研究

Adjudin is a potent blocker of Cl     ^-    channels: disrupting Cl     ^-    ion transport function results in a decline in sperm capacitation and fertilizing ability in humans in vitro. Adjudin (ADD) is a mitochondria inhibitor. Adjudin is a molecule that mediates adherens junction disruption at the Sertoli-germ cell interface. To investigate the effect of Adjudin on cancer cells, more than ten different types of human or mice cancer cell lines are treated with increasing concentrations of Adjudin and the cell proliferation is measured by the modified MTT assay. Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinoma cell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC     ₅₀    of Adjudin is determined to be 58.0 μM, 13.8 μM, 72.3 μM and 52.7 μM against SGC-7901, MDA-MB-231, Smmc-7721 and MIA Paca-2 cells, respectively, after treatment for 24 h. Similar results are obtained in other human and mice cancer cell lines. The IC     ₅₀    of Adjudin in A549 cells and PC3 cells is 63.1 μM and 93.0 μM, respectively. For WI-38 and BPH-1 cells, the IC     ₅₀    of Adjudin can be observed at more than 300 μM and 200 μM, respectively, which is about 5 times and 2 times more than that for the cancer cell lines A549 and PC3.

體內(nèi)研究

To determine whether Adjudin can inhibit lung and prostate cancer growth in vivo, the effect of Adjudin is tested in a subcutaneous model of lung and prostate cancer. Human lung carcinoma cells A549 and prostate carcinoma cells PC3 are injected into athymic nude mice subdermally at the lower back site respectively. Mice are then randomized into two treatment groups with similar mean tumor sizes: Adjudin and vehicle (control). Approximately 2 weeks after tumor inoculation Adjudin is injected intraperitoneally once every three days in lung carcinoma cells and every other day in prostate carcinoma cells at 100 mg/kg. Adjudin treatment can be well tolerated in rodent. And Adjudin-treated mice show significant tumor growth inhibition compared with the control group (P<0.0001 in the human lung carcinoma cells A549 and P=0.006 in the prostate carcinoma cells PC3).

安全信息

MSDS信息

1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼 價格(試劑級)

1-(2,4-二氯芐基)-1H-吲唑-3-碳酰肼 上下游產(chǎn)品信息

上游原料

1H-INDAZOLE-3-CARBOXYLIC ACID, 1-[(2,4-DICHLOROPHENYL)METHYL]-, METHYLESTER