靶点：NF-κB 通路：NF-κB 背景说明：Pyrrolidinedithiocarbamate Ammonium是选择性的 NF-κB 抑制剂。 生物活性：Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate) is a selective and blood-brain barrier (BBB) permeable NF-κB inhibitor.[1-2] In Vitro：Pretreatment of cells with Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate; 3-1000 μM) dose-dependently attenuate IL-8 production[1]. Furthermore， pyrrolidinedithiocarbamate ammonium (100 μM) suppresses the accumulation of IL-8 mRNA[1]. Pyrrolidinedithiocarbamate ammonium inhibits the activation of NF-κB， because it suppresses both NF-κB DNA binding and NF-κB-dependent transcriptional activity. NF-κB inhibition with pyrrolidinedithiocarbamate ammonium decrease IL-8 production by intestinal epithelial cells[1]. In Vivo：The DSS+pyrrolidinedithiocarbamate ammonium-treated groupII exhibits suppression of shortening of intestinal length and reduction of DAI score. Activated NF-κB level and IL-1β and TNF-α levels are significantly lower in DSS+pyrrolidinedithiocarbamate ammonium-treated groupII. These findings suggest that suppression of NF-κB activity by pyrrolidinedithiocarbamate ammonium can delay the healing of mucosal tissue defects (erosions or ulcers) arising from inflammation， but that it can strongly suppress the expression of inf-lammatory cytokines (IL-1β and TNF-α)， resulting in significant alleviation of colitis. pyrrolidinedithiocarbamate ammonium is useful for the treatment of ulcerative colitis[2]. 细胞实验：The human colon cancer cell line HT-29 is obtained and cells are grown in modified McCoy’s 5A medium supplemented with 10% fetal bovine serum. To study the effect of pyrrolidinedithiocarbamate ammonium on IL-8 production， HT-29 cells in 96-well plates are induced with 20 ng/mL of IL-1β for 18 h. Various concentrations (3-1000 μM) of pyrrolidinedithiocarbamate or its vehicle (culture medium) are added to the cells 30 min prior to IL-1β stimulation. The concentration of IL-8 in the supernatant is determined using solid-phase enzyme-linked immunosorbent assay[1]. 动物实验：Animal Administration: [2]Pyrrolidinedithiocarbamate is administered intraperitoneally to mice at dose levels of 100 and 50 mg/kg. Mice are divided into a DSS-untreated group (normal group)， DSS-treated control group， DSS+pyrrolidinedithiocarbamate-treated groupI (low-dose group)， and DSS+pyrrolidinedithiocarbamate-treated groupII (high-dose group). In each group， the disease activity index score (DAI score)， intestinal length， histological score， and the levels of activated NF-κB and inflammatory cytokines (IL-1β and TNF-α) in tissue are measured[2]. 数据来源文献：[1]. Németh ZH， et al. Pyrrolidinedithiocarbamate inhibits NF-kappaB activation and IL-8 production in intestinal epithelial cells. Immunol Lett. 2003 Jan 2;85(1):41-6. [2]. Qin JD， et al. Effect of ammonium pyrrolidine dithiocarbamate (PDTC) on NF-κB activation and CYP2E1 content of rats with immunological liver injury. Pharm Biol. 2014 Nov;52(11):1460-1466.
基本信息：
CAS：5108-96-3 中文名称：吡咯烷二硫代氨基甲酸铵(10mM in DMSO,无菌） 英文名称：Pyrrolidinedithiocarbamate Ammonium(10mM in DMSO,Sterile） 分子式：C5H9NS2·NH3 分子量：164.29 规格：1ml ; 1.5ml ; 0.5ml ; 0.3ml ; 0.1ml 溶解性：请根据自己的实验要求使用。 外观(性状)：无菌溶液 储存条件：Stroe at -20℃，6 months.
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