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Pyrrolidinedithiocarbamate ammonium

MCE China：Pyrrolidinedithiocarbamate ammonium

Brand：MedChemExpress (MCE)

Cat. No.HY-18738

CAS：5108-96-3

Synonyms：Ammonium pyrrolidinedithiocarbamate; PDTC ammonium; APDC

Purity：98.0%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate) is a selective and blood-brain barrier (BBB) permeable NF-κB inhibitor.

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].

Animal Administration：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].

Cell Assay：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].

IC50 & Target：NF-κB

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References：

[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.  [Content Brief]

[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.  [Content Brief]