Prim-O-glucosylcimifugin - NO Synthase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPrim-O-glucosylcimifuginCat. No.: HY-N0635CAS No.: 80681-45-4分式: CHO分量: 468.45作靶點(diǎn): NO Synthase; COX作通路: Immunology/Inflammation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)

2、DMSO : 150 mg/mL (320.20 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.1347 mL 10.6735 mL 21.3470 mL5 mM 0.4269 mL 2.1347 mL 4.2694 mL10 mM 0.2135 mL 1.0673 mL 2.1347 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 Prim-O-glucosy

3、lcimifugin 具有強(qiáng)效的抗炎作。通過調(diào)節(jié) JAK2/STAT3 信號(hào)傳導(dǎo)可抑制 iNOS 和 COX-2 表達(dá)。IC50 & Target COX-2 iNOS體外研究Prim-O-glucosylcimifugin (POG) is the highest content chromone and one of the major active constituents inRadix Saposhnikoviae (RS). Prim-O-glucosylcimifugin exerts anti-inflammatory effects in RAW 264.7macrophag

4、es through the inhibition of iNOS and COX-2 expression by inhibiting JAK2/STAT3 signaling. The1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEcytotoxicity of Prim-O-glucosylcimifugin is measured to LPS-activated Raw 264.7 macrophages. Raw 264.7macrophages are treated with LPS (1 g/mL) and increasin

5、g concentrations of Prim-O-glucosylcimifugin (15,50, and 100 g/mL) for 24 h and cell viability is evaluated by CCK-8 assay. Cell viability is not significantlyaffected after 24 h and exposure to 15-100 g/mL Prim-O-glucosylcimifugin as compared with DMSO-treatedcells (control). To investigate the ant

6、i-inflammatory effect of Prim-O-glucosylcimifugin, whether Prim-O-glucosylcimifugin can affect NO synthesis is examined in LPS-activated RAW 264.7 cells. Macrophages aretreated with LPS (1 g/mL) and various concentrations of Prim-O-glucosylcimifugin (15, 50, and 100 g/mL)for 24 h. No concentrations

7、are measured in the culture supernatants by Griess reaction. The concentrationsof NO in the culture supernatants are markedly increased in response to LPS exposure, and Prim-O-glucosylcimifugin significantly inhibits LPS-induced NO production in a concentration-dependent manner 1.體內(nèi)研究 Bronchoalveola

8、r lavage fluid (BALF) is collected at 7 h after lipopolysaccharide (LPS) administration andthecytokine levels in BALF are measured by ELISA. The levels of TNF-, IL-1 and IL-6 in BALF areincreased dramatically compared with control group. However, pretreatment with Prime-O-glucosylcimifugin(2.5, 5 or

9、 10 mg/kg) significantly down-regulates the levels of TNF-, IL-1 and IL-6 in a dose-dependentmanner (P 1.PROTOCOLCell Assay 1 Cell Counting Kit (CCK-8) is used to determine the cytotoxic concentrations of Prim-O-glucosylcimifugin. Inbrief, the Raw 264.7 cells are plated at a density of 1104 cells pe

10、r well in a 96-well and incubated overnight.Cells are then stimulated with 1 g/mL LPS and treated with various concentrations of Prim-O-glucosylcimifugin (15, 50, and 100 g/mL; MedChem Express, Princeton, NJ, USA) or DMSO. Afterincubation at 37C for 24 h, CCK-8 solution is added to each well and inc

11、ubated for another 1 h. Theabsorbance is measured at 450 nm using a microplate reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 BALB/c male mice, 8 weeks old and weighing approximately 18 to 20 g, are used. The mice

12、 are randomlydivided into five groups: Control group; LPS group; LPS+Prime-O-glucosylcimifugin (2.5, 5 or 10 mg/kgbodyweight). Prime-O-glucosylcimifugin is given intraperitoneally. One hour later, LPS group andLPS+Prime-O-glucosylcimifugin group mice are given 50 L LPS intranasally (i.n) (200 mg/L)

13、to induce acutelung injury. Control mice are given 50 L PBS intranasally (i.n) without LPS 1.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) Pharmacogn Mag. 2017 Jul-Sep;13(51):378-384.See more customer validations on HYPERLINK / www.MedChem

14、EREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Zhou J, et al. Prim-O-glucosylcimifugin Attenuates Lipopolysaccharideinduced Inflammatory Response in RAW 264.7 Macrophages.Pharmacogn Mag. 2017 Jul-Sep;13(51):378-384.2. Chen N, et al. Prime-O-glucosylcimifugin attenuates lipopolysaccharide-induced acute lung injury in mice. Int Immunopharmacol. 2013Jun;1