Homoplantaginin - TNF Receptor 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEHomoplantagininCat. No.: HY-N1949CAS No.: 17680-84-1分式: CHO分量: 462.4作靶點: TNF Receptor; NF-B作通路: Apoptosis; NF-B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 : 100 mg/mL (216.26 mM)* means s

2、oluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1626 mL 10.8131 mL 21.6263 mL5 mM 0.4325 mL 2.1626 mL 4.3253 mL10 mM 0.2163 mL 1.0813 mL 2.1626 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 Homoplantaginin來中藥Salvia plebeia的具有抗炎和抗氧化活性的類酮。IC50

3、 & Target TNF- p65體外研究Homoplantaginin shows IC50 of reduction level of DPPH radical at 0.35 g/mL. In human hepatocyte HL-7702 cells exposed to H2O2, the addition of 0.1-100g/mL of homoplantaginin significantly reduces lactate1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEdehydrogenase leakage, and

4、 increases glutathione, glutathione peroxidase and superoxide dismutase insupernatant 1. Homoplantaginin (0.1, 1, 10 M) dose-dependently reduces expression of toll-like receptor-4evoked by palmitic acid (100 M). Homoplantaginin tightly controlls palmitic acid-induced reactive oxygenspecies to preven

5、t nucleotide-binding domain-like receptor 3 (NLRP3) inflammasome activation bysuppressing reactive oxygen species-sensitive thioredoxin-interacting protein, NLRP3, and caspase-1 2.Pre-treatment of homoplantaginin on human umbilical vein endothelial cells significantly inhibits palmitic acidinduced T

6、NF- and IL-6 mRNA expression, and IKK and NF-B p65 phosphorylation. Homoplantagininsignificantly modulates the Ser/Thr phosphorylation of IRS-1, improves phosphorylation of Akt andendothelial nitric oxide synthase, and increases NO production in the presence of insulin 3.體內(nèi)研究 Homoplantaginin(25-100m

7、g/kg) significantly reducesthe increase in serum alanine aminotranseferase andaspartate aminotransferase, decreases the levels of TNF- and IL-1. The same treatment also reduces thecontent of thiobarbituric acid-reactive substances, elevates the levels of GSH, GSH-Px and SOD in hepatichomogenate 1. H

8、omoplantaginin is rapidly absorbed (Tmax=16.008.94min), reaching a mean Cmaxbetween 0.77 and 1.27nmol/mL. The absolute oral bioavailability is calculated to be only 0.75%.PROTOCOLCell Assay 3 The viability of cultured cells is determined using the MTT assay. Human umbilical vein endothelial cells ar

9、eexposed to various concentrations of homoplantaginin (0.1, 1, 3, 10, 30, 100 M) for 48 h. Subsequently, 20L of MTT (5 mg/mL) is added to each well for an additional 4 h at 37C. The supernatant is removed, andDMSO is added to dissolvethe formazan crystals. The optical absorbance is measured at 540 n

10、m 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: Homoplantaginin is dissolved in a solution consistingof DMSO, PEG 400, ethanol and normalAdministration 14 saline(2:2:3:3, v/v/v/v) at a concentration of 10 mg/mL. The rats are randomly di

11、vided into three groups toreceive oral administration(150 mg/kg), tail vein injection (15 mg/kg) and peritoneal injectionv (15 mg/kg).Blood samples (approximately 0.5 mL) are collected from the retro-orbital plexus into heparinizedmicrofugetubes at 5, 10, 20, 30, 45, 60, 90, 120, and 180 min after a

12、dministration. The plasma samples,separated by centrifuging the blood samples at 10,000 rpm 4.Mice: Homoplantaginin is dissolved in 5% amylum. Homoplantaginin is administered orally by gastricintubation during the experimental period at doses of 25, 50, 100 mg/kg/d, respectively. Eight hours afterin

13、jection of LPS, the mice are anesthetized with ether and blood samples are collected by exsanguinationfrom the inferior vein. The liver is removed and fixed in formalin for histological analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENC

14、ES1. Qu XJ, et al. Protective effects of Salvia plebeia compound homoplantaginin on hepatocyte injury. Food Chem Toxicol. 2009Jul;47(7):1710-5.2. He B, et al. Homoplantaginin Inhibits Palmitic Acid-induced Endothelial Cells Inflammation by Suppressing TLR4 and NLRP3Inflammasome. J Cardiovasc Pharmac

15、ol. 2016 Jan;67(1):93-101.3. Wu F, et al. Homoplantaginin modulates insulin sensitivity in endothelial cells by inhibiting inflammation. Biol Pharm Bull.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2012;35(7):1171-7.4. Cong Y, et al. Pharmacokinetics of homoplantaginin in rats following intravenous, peritoneal injection and oral administration. J PharmBiomed