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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENeferineCat. No.: HY-N0441CAS No.: 2292-16-2Synonyms: (-)-Neferine分式: CHNO分量: 624.77作靶點(diǎn): NF-B; Autophagy作通路: NF-B; Autophagy儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMS
2、O : 62 mg/mL (99.24 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6006 mL 8.0029 mL 16.0059 mL5 mM 0.3201 mL 1.6006 mL 3.2012 mL10 mM 0.1601 mL 0.8003 mL 1.6006 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)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Neferine種雙芐 異喹啉類物堿。Neferine 強(qiáng)效抑制 NF-B 激活。IC
3、50 & Target p65 Autophagy體外研究Neferine down regulates hypoxia induced NF-B p65 nuclear translocation and COX-2 expressions 1.Neferine reduces high-glucose-induced collagen production and inhibits TGF-1-Smad, ERK and p38 MAPKsignaling activation in cardiac fibroblasts. Cardiac fibroblasts (CFs) are cu
4、ltured in HG medium with varying1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEconcentrations of Neferine (1, 2, or 5 M). CCK-8 assays are carried out at different time points (24, 48, and72 h). Compared with normal glucose (NG) and osmotic control (OC) treatments, High glucose (30 mM)treatment si
5、gnificantly increases the proliferation of CFs in a time-dependent manner (P 2.體內(nèi)研究 Neferine treatment at both low-dose (60 mg/kg/day by gavage) and high-dose (120 mg/kg/day by gavage)reduces the increment of collagen I, III and TGF-1 protein expression induced by hyperglycemia 2.PROTOCOLCell Assay
6、2 Cardiac fibroblasts (CFs) are isolated from neonatal mouse ventricular tissues. After starvation in serum-freemedium for 24 h, CFs are incubated in DMEM containing 5.6 mM glucose (normal glucose; NG), 30 mM D-glucose (HG), 30 mM D-glucose plus 1 M Neferine, 30 mM D-glucose plus 2 M Neferine, 30 mM
7、 D-glucose plus 5 M Neferine, and 5.6 mM glucose plus 27.5 mM mannose. Cells are harvested at 24 h, 48 h,and 72h. Cell proliferation is measured with the Cell Counting Kit-8 (CCK-8) and the Cell-LightTM EdU assay2.MCE has not independently confirmed the accuracy of these methods. They are for refere
8、nce only.Animal Mice 2Administration 2 Eight-week-old C57BL/6J male mice are used. Diabetes is induced by intraperitoneal injection ofStreptozotocin dissolved in citrate buffer (pH 4.5) at 60 mg/kg body weight for five consecutive days. Controlmice are injected with citrate buffer only. Whole blood
9、glucose in mouse tail blood is detected with an Accu-Check Active glucometer. Mice with blood glucose concentrations higher than 18 mM are considered asdiabetic animals and used in this study. The animals are randomly divided into four groups of eight animalseach. Diabetic mice are divided into thre
10、e groups: group 1, the diabetic control group (DM); group 2, whichreceive Neferine at a dose of 60 mg/kg/day (DM-NL); and group 3, which receive Neferine at a dose of 120mg/kg/day (DM-NH). Neferine is administered twice per day by intragastric gavage for 12 weeks. Equivalentvolumes of normal sodium
11、are administered to the normal and DM control groups by gavage. Mice areanaesthetized and sacrificed at the end of the 12-week treatment 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Inflamm Res. 2019 Jun 6.See more customer validations
12、on HYPERLINK / www.MedChemEREFERENCES1. Baskaran R, et al. Neferine prevents NF-B translocation and protects muscle cells from oxidative stress and apoptosis induced byhypoxia. Biofactors. 2016 Jul 8;42(4):407-17.2. Liu X, et al. Neferine inhibits proliferation and collagen synthesis induced by high glucose in cardiac fibroblasts and reduces cardiacfibrosis in diabetic mice. Oncotarget. 2016 Sep 20;7(38):61703-61715.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEC
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