Gentiopicroside-Gentiopicrin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGentiopicrosideCat. No.: HY-N0494CAS No.: 20831-76-9Synonyms: Gentiopicrin分式: CHO分量: 356.32作靶點: Cytochrome P450作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO :

2、150 mg/mL (420.97 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8065 mL 14.0323 mL 28.0647 mL5 mM 0.5613 mL 2.8065 mL 5.6129 mL10 mM 0.2806 mL 1.4032 mL 2.8065 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，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Gentiopicroside種天然的環(huán)烯

3、醚萜苷，能夠抑制 P450 的活性，對 CYP2A6 的 IC50 和 Ki 值分別為 61 M和 22.8 M；Gentiopicroside 具有抗炎和抗氧化活性。IC50 & Target IC50: 61 M (CYP2A6) 1Ki: 22.8 M (CYP2A6) 11/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Gentiopicroside inhibits P450 activity, with an IC50 and a Ki of 61 M and 8.12 M for CYP2A6, also slightly

4、inhibits CYP2E1 activity with an IC50 of 1.6 mM, but shows no inhibition on CYP1A2 and CYP3A4 1.Gentiopicroside (12.5, 25 and 50M) inhibits RANKL-induced osteoclast formation from mouse bone marrowmacrophages (BMMs) in a dose-dependent manner, blocks the expression of osteoclast-related proteins,pre

5、vents receptor activator of nuclear factor-B ligand (RANKL)-triggered JNK and NF-B activation.Gentiopicroside (50M) also inhibits RANKL-induced bone resorption 3.體內(nèi)研究 Gentiopicroside (20, 40, and 80 mg/kg, p.o.) significantly reduces gastric ulcerindex in mice. Gentiopicroside(20, 40, and 80 mg/kg)

6、also ovbiously decreases the levels of HSP-70, TNF-, IL-6, MDA and increasesncreased GSH level and SOD activity. In addition, Gentiopicroside normalizes EGF and VEGF level in mice2.PROTOCOLCell Assay 3 Cell viability is evaluated using the CCK-8 assay. In brief, bone marrow macrophages (BMMs) (1104c

7、ells/well) are placed in a 96-well plate and cultured with various concentrations of Gentiopicroside (12.5, 25and 50 M) for 48 h in the presence of M-CSF (30 ng/mL) and RANKL (100 ng/mL). Then, 10 L of theCCK-8 solution is added to each well and the mixture is incubated for 4 h at 37C. The absorbanc

8、e isevaluated at 450 nm using a microplate reader 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 Mice are ran-domLy divided into six groups with 10 animals each. Drug is given by intragastric administrationonce a day for

9、 three consecutive days. Mice in the normal control group and the ethanol control group(negative control) receive saline at a dose of 2.5 mL/kg; Mice in the cimetidine control group (positive control)receive cimetidine at a dose of 100 mg/kg; mice in three Gentiopicroside investigative groups receiv

10、edifferent doses of Gentiopicroside (20, 40, and 80 mg/kg), respectively; On the third day, except that mice inthe normal control group receive saline, mice in other groups receive 70% ethanol at a dose of 0.01 mL/g byoral1 hr after the last intragastric administration. One hour after the induction,

11、 animals are euthanized underanesthesia by cervical dislocation, removed and cut the stomach longitudinally. The stomach are openedalong the greater curvature and rinsed slightly with ice-cold saline to remove the gastric contents, and thenthe severity of gastric mucosal injury is evaluated by gastr

12、ic ulcer index. Subsequently, eachanimalsstomach is cut into two moieties, with one moiety of stomach stored at 80C for biochemicalassessment and the other moiety immersed in 4% paraformaldehyde solution for histopathologicalexaminations 2.MCE has not independently confirmed the accuracy of these me

13、thods. They are for reference only.REFERENCES1. Deng Y, et al. In vitro inhibition and induction of human liver cytochrome P450 enzymes by gentiopicroside: potent effect on CYP2A6.Drug Metab Pharmacokinet. 2013;28(4):339-44. Epub 2013 Feb 19.2. Yang Y, et al. Protective effect of gentiopicroside fro

14、m Gentiana macrophylla Pall. in ethanol-induced gastric mucosal injury in mice.Phytother Res. 2018 Feb;32(2):259-266.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Chen F, et al. Gentiopicroside inhibits RANKL-induced osteoclastogenesis by regulating NF-B and JNK signaling pathways. BiomedPharmacother. 2018 Apr;10