1、Product Data SheetNeferineCat. No.: HY-N0441CAS No.: 2292-16-2分式: CHNO分量: 624.77作靶點(diǎn): NF-B; Autophagy; Apoptosis作通路: NF-B; Autophagy; Apoptosis儲(chǔ)存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 62 mg/mL (99.24 mM; Need ultrasonic)SolventMass1

2、mg 5 mg 10 mgConcentration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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)

3、物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.33 mM); Clear solution此案可獲得 2.08 mg/mL (3.33 mM，飽和度未

4、知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.33 mM); Clear solution此案可獲得 2.08 mg/mL (3.33 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMS

5、O 儲(chǔ)備液加到 900 L 油中，混合均勻。Page 1 of 2 www.MedChemEBIOLOGICAL 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 & Target p65 Autophagy體外研究 Neferine down regulates hypoxia induced NF-B p65 nuclear translocation and COX-2 expressions1. Neferinereduces high-glucose-induced collagen production and inhi

6、bits TGF-1-Smad, ERK and p38 MAPK signalingactivation in cardiac fibroblasts. Cardiac fibroblasts (CFs) are cultured in HG medium with varying concentrations ofNeferine (1, 2, or 5 M). CCK-8 assays are carried out at different time points (24, 48, and 72 h). Compared withnormal glucose (NG) and osmo

7、tic control (OC) treatments, High glucose (30 mM) treatment significantly increases theproliferation of CFs in a time-dependent manner (P0.05). High glucose (HG)-induced CF proliferation is markedlyattenuated by Neferine treatment at either 2 or 5 M compared with vehicle treatment. However, 1 M Nefe

8、rine doesnot inhibit HG-induced proliferation of CFs. Therefore, 2 and 5 M Neferine are used in the remaining experiments2.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) reducesthe increment of collagen I, III and TGF-1 protein expression in

9、duced by hyperglycemia2.PROTOCOLCell Assay 2 Cardiac fibroblasts (CFs) are isolated from neonatal mouse ventricular tissues. After starvation in serum-free mediumfor 24 h, CFs are incubated in DMEM containing 5.6 mM glucose (normal glucose; NG), 30 mM D-glucose (HG), 30mM D-glucose plus 1 M Neferine

10、, 30 mM D-glucose plus 2 M Neferine, 30 mM 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 measuredwith the Cell Counting Kit-8 (CCK-8) and the Cell-LightTM EdU assay2.MCE has not independently confirmed the accur

11、acy of these methods. They are for reference only.Animal Mice2Administration 2 Eight-week-old C57BL/6J male mice are used. Diabetes is induced by intraperitoneal injection of Streptozotocindissolved in citrate buffer (pH 4.5) at 60 mg/kg body weight for five consecutive days. Control mice are inject

12、ed withcitrate buffer only. Whole blood glucose in mouse tail blood is detected with an Accu-Check Active glucometer. Micewith blood glucose concentrations higher than 18 mM are considered as diabetic animals and used in this study. Theanimals are randomly divided into four groups of eight animals e

13、ach. Diabetic mice are divided into three groups:group 1, the diabetic control group (DM); group 2, which receive Neferine at a dose of 60 mg/kg/day (DM-NL); andgroup 3, which receive Neferine at a dose of 120 mg/kg/day (DM-NH). Neferine is administered twice per day byintragastric gavage for 12 wee

14、ks. Equivalent volumes of normal sodium are administered to the normal and DMcontrol groups by gavage. Mice are anaesthetized and sacrificed at the end of the 12-week treatment2.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. 20

15、19 Jun 6. Inflammation. 2020 Jun 2. Int J Neurosci. 2020 May 7:1-11.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Baskaran R, et al. Neferine prevents NF-B translocation and protects muscle cells from oxidative stress and apoptosis induced by hypoxia. 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 cardiac fibrosis in diabeticmice. Oncotarget. 2016 Sep 20;7(