Peretinoin-NIK333-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPeretinoinCat. No.: HY-100008CAS No.: 81485-25-8Synonyms: NIK333分式: CHO分量: 302.45作靶點(diǎn): RAR/RXR; SPHK; Autophagy; HCV作通路: Metabolic Enzyme/Protease; Immunology/Inflammation;Autophagy; Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yea

2、rsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (330.63 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.3063 mL 16.5317 mL 33.0633 mL5 mM 0.6613 mL 3.3063 mL 6.6127 mL10 mM 0.3306 mL 1.6532 mL 3.3063 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意

3、儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Peretinoin種服環(huán)狀類視 醇，具有類維素 A 結(jié)構(gòu)，靶向類視黃醇核受體，例如 RXR 和 RAR。Peretinoin 通過下調(diào)轉(zhuǎn)錄因 Sp1，在體外降低 SPHK1 的 mRNA 平。 Peretinoin 通過增加 Atg16L1 表達(dá)激活噬途徑，防酒精性脂肪性肝炎 (NASH) 和肝細(xì)胞癌 (HCC) 的發(fā)展。Peretinoin 通過改變脂質(zhì)代謝來抑制 HCV RNA 擴(kuò)增和病毒釋放，EC50 為 9 M。1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEIC50

4、 & Target RAR RXR體外研究 Peretinoin (5M; 24hours) up-regulates the expression of LC3B-II and increases autophagy flux in mouseprimary hepatocytes 2.Peretinoin (10-40M; 12-72hours) exhibits suppressed SPHK1 expression after 24h treatment, even at 10M and more prominent after 72 h peretinoin treatment 1.

5、Cell Autophagy Assay 2Cell Line: Mouse primary hepatocytes (MPH) and the human HCC HepG2 cell lineConcentration: 5MIncubation Time: 24 hoursResult: Up-regulated the expression of LC3B-II and increased autophagy flux.Western Blot Analysis 1Cell Line: Human hepatoma (Huh-7) cellsConcentration: 10, 20

6、and 40MIncubation Time: 12, 24, 48 and 72 hoursResult: Exhibited suppressed SPHK1 expression after 24h treatment, even at 10M.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Antivir Res. 2019 Jul.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Funaki M, et al. Peretinoin, an acyclic retinoid, inhibits hepatocarci

7、nogenesis by suppressing sphingosine kinase 1 expression in vitroand in vivo. Sci Rep. 2017 Dec 5;7(1):16978.2. Okada H, et al. Peretinoin, an acyclic retinoid, suppresses steatohepatitis and tumorigenesis by activating autophagy in mice fed anatherogenic high-fat diet. Oncotarget. 2017 Jun 20;8(25):39978-39993.3. Honda M, et al. Peretinoin, an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy ofhepatocellular carcinoma. BMC Cancer. 2013 Apr 15;13:191.McePdfHeightCaution: Product has not been fully validated for medical applications.For