Osalmid-Oxaphenamide-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOsalmidCat. No.: HY-B2116CAS No.: 526-18-1Synonyms: Oxaphenamide; 4-Hydroxysalicylanilide分式: CHNO分量: 229.23作靶点: HBV作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 28 mg/m

2、L (122.15 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.3624 mL 21.8122 mL 43.6243 mL5 mM 0.8725 mL 4.3624 mL 8.7249 mL10 mM 0.4362 mL 2.1812 mL 4.3624 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Osalmid核糖核苷酸还原酶亚基M2（RRM2）的靶向化

3、合物；抑制核糖核苷酸还原酶活性的IC50值为8.23M。IC50 & Target IC50: 8.23 M (ribonucleotide reductase) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Osalmid is identified as a potential ribonucleotide reductase small subunit M2 (RRM2) compound. Osalmid is10-fold more active in inhibiting ribonucleotide reductas

4、e (RR) activity than hydroxyurea, and significantlyinhibits HBV DNA and cccDNA synthesis in HepG2.2.15 cells in a time- and dose-dependent manner. Aftertreatment for 8 days with Osalmid, the EC50 for HBV DNA inhibition are 11.1 M for culture supernatant and16.5 M for cells. Osalmid suppresses RR act

5、ivity in a concentration-dependent manner, with an IC50 of8.23 M. Osalmid is shown to possess potent activity against a 3TC-resistant HBV strain, suggesting utility intreating drug-resistant HBV infections 1.体内研究 Osalmid reduces RR activity and HBV replication in HBV-transgenic mice and shows a syne

6、rgistic efficacywith 3TC without significant toxicity. Oral dosing of osalmid at 400 mg/kg/d results in a time-dependentinhibition of HBV DNA replication. After treatment for 4 weeks, osalmid suppresses HBV DNA replication byabout 40-45% as compared to the control in mouse sera and liver tissues 1.P

7、ROTOCOLCell Assay 1 HepG2.2.15 cells are cultured in the presence of 200 g/mL G418. Cell viability is determined using a CellCounting Kit-8 in 96-well plates treated with Osalmid for designated times. For long term assays, the culturesupernatants are replaced with fresh media containing Osalmid ever

8、y two days. The control wells containedequivalent amounts of DMSO. The CC50 is calculated as the concentration of a compound that reduced thecell viability to 50% compared to the control 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: The

9、 HBV-transgenic mouse lineage is initially produced on a BALB/c background. Osalmid or 3TC isAdministration 1 suspended in 0.05% CMC-Na and administered once a day by gavage at 400 and 100 mg/kg, respectively,for 28 days. For the combination group, mice are intragastrically administered with a mixtu

10、re of osalmid and3TC. 0.05% CMC-Na solution is used as control. The mouse sera are collected and assayed for HBV DNAlevels and AST/ALT activity. Mice are then sacrificed after the 28-day drug treatment and the livers areexcised for analysis 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Liu X, et al. Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochem Pharmacol. 2016 Mar1;103:118-28.McePdfHeightCaution: Product has not been