吡咯烷二硫代甲酸銨鹽作用機制 - Medchemexpress - MCE中國

1、Product Data SheetPyrrolidinedithiocarbamate ammoniumCat. No.: HY-18738CAS No.: 5108-96-3分式: CHNS分量: 164.29作靶點: NF-B作通路: NF-B儲存式: Powder -20°C 3 years4°C 2 yearsIn solvent -80°C 6 months-20°C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 42 mg/mL (255.65 mM)* "" means soluble, but saturation

2、 unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 6.0868 mL 30.4340 mL 60.8680 mL5 mM 1.2174 mL 6.0868 mL 12.1736 mL10 mM 0.6087 mL 3.0434 mL 6.0868 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個內(nèi)使，-20°C

3、 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (12.66 mM); Clear solution此案可獲得 2.08 m

4、g/mL (12.66 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (12.66 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.08 mg/mL (12.66 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 20.8 mg/mL

5、 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate)是選擇性的 NF-B 抑制劑。IC & Target NF-B體外研究 Pretreatment of cells with Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate; 3-1000 M) dose-dependently attenua

6、te IL-8 production1.Furthermore, pyrrolidinedithiocarbamate ammonium (100 M) suppresses the accumulation of IL-8 mRNA1.Pyrrolidinedithiocarbamate ammonium inhibits the activation of NF-B, because it suppresses both NF-B DNAbinding and NF-B-dependent transcriptional activity. NF-B inhibition with pyr

7、rolidinedithiocarbamate ammoniumdecrease IL-8 production by intestinal epithelial cells1.體內(nèi)研究 The DSS+pyrrolidinedithiocarbamate ammonium-treated groupII exhibits suppression of shortening of intestinallength and reduction of DAI score. Activated NF-B level and IL-1 and TNF- levels are significantly

8、 lower in DSS+pyrrolidinedithiocarbamate ammonium-treated groupII. These findings suggest that suppression of NF-Bactivity by pyrrolidinedithiocarbamate ammonium can delay the healing of mucosal tissue defects (erosions or ulcers)arising from inflammation, but that it can strongly suppress the expre

9、ssion of inf-lammatory cytokines (IL-1 andTNF-), resulting in significant alleviation of colitis. pyrrolidinedithiocarbamate ammonium is useful for the treatmentof ulcerative colitis2.PROTOCOLCell Assay 1 The human colon cancer cell line HT-29 is obtained and cells are grown in modified McCoys 5A me

10、diumsupplemented with 10% fetal bovine serum. To study the effect of pyrrolidinedithiocarbamate ammonium on IL-8production, HT-29 cells in 96-well plates are induced with 20 ng/mL of IL-1 for 18 h. Various concentrations (3-1000M) of pyrrolidinedithiocarbamate or its vehicle (culture medium) are add

11、ed to the cells 30 min prior to IL-1stimulation. The concentration of IL-8 in the supernatant is determined using solid-phase enzyme-linkedimmunosorbent assay1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Animal Administration: 2Pyrrolidinedit

12、hiocarbamate is administered intraperitoneally to mice at dose levels of 100Administration 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-treatedgro

13、upII (high-dose group). In each group, the disease activity index score (DAI score), intestinal length, histologicalscore, and the levels of activated NF-B and inflammatory cytokines (IL-1 and TNF-) in tissue are measured2.MCE has not independently confirmed the accuracy of these methods. They are f

14、or reference only.戶使本產(chǎn)品發(fā)表的科研獻 J Exp Med. 2020 Jul 6;217(7). pii: e20192083. Cell Death Dis. 2019 Feb 8;10(2):113.Page 2 of 3 www.MedChemE Pharmacol Res. 2018 Jul;133:218-235. Oncoimmunology. 2018 Aug 23;7(11):e1461303. Oxid Med Cell Longev. 2017;2017:3869561.See more customer validations on www.MedC

15、hemEREFERENCES1. Németh ZH, et al. Pyrrolidinedithiocarbamate inhibits NF-kappaB activation and IL-8 production in intestinal epithelial cells. Immunol Lett. 2003 Jan2;85(1):41-6.2. Qin JD, et al. Effect of ammonium pyrrolidine dithiocarbamate (PDTC) on NF-B activation and CYP2E1 content of rats with immunological liver injury.Pharm Biol. 2014 Nov;52(11):146