Osalmid (Oxaphenamide)
(Synonyms: 羟苯水杨胺; Oxaphenamide; 4'-Hydroxysalicylanilide) 目录号 : GC32144Osalmid suppresses ribonucleotide reductase (RNR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM.
Cas No.:526-18-1
Sample solution is provided at 25 µL, 10mM.
Osalmid suppresses ribonucleotide reductase (RNR) activity in a concentration-dependent manner, with a 50% RR activity-inhibitory concentration (IC50) of 8.23 μM.
Osalmid is shown to be 10-fold more active in inhibiting RR activity than hydroxyurea, and significantly inhibits HBV DNA and cccDNA synthesis in HepG2.2.15 cells. Osalmid significantly inhibits HBV DNA replication in a time- and dose-dependent manner[1].
Osalmid significantly reduces RR activity and HBV DNA replication in vivo[1].
[1] Liu X, et al. Biochem Pharmacol. 2016, 103:118-28.
Cell experiment: | HepG2.2.15 cells are cultured in the presence of 200 μg/mL G418. Cell viability is determined using a Cell Counting Kit-8 in 96-well plates treated with Osalmid for designated times. For long term assays, the culture supernatants are replaced with fresh media containing Osalmid every two days. The control wells contained equivalent amounts of DMSO. The CC50 is calculated as the concentration of a compound that reduced the cell viability to 50% compared to the control[1]. |
Animal experiment: | Mice: The HBV-transgenic mouse lineage is initially produced on a BALB/c background. Osalmid or 3TC is 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 mixture of osalmid and 3TC. 0.05% CMC-Na solution is used as control. The mouse sera are collected and assayed for HBV DNA levels and AST/ALT activity. Mice are then sacrificed after the 28-day drug treatment and the livers are excised for analysis[1]. |
References: [1]. Liu X, et al. Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochem Pharmacol. 2016 Mar 1;103:118-28. |
Cas No. | 526-18-1 | SDF | |
别名 | 羟苯水杨胺; Oxaphenamide; 4'-Hydroxysalicylanilide | ||
Canonical SMILES | O=C(NC1=CC=C(O)C=C1)C2=CC=CC=C2O | ||
分子式 | C13H11NO3 | 分子量 | 229.23 |
溶解度 | DMSO : ≥ 28 mg/mL (122.15 mM) | 储存条件 | Store at -20°C |
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制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.3624 mL | 21.8122 mL | 43.6243 mL |
5 mM | 0.8725 mL | 4.3624 mL | 8.7249 mL |
10 mM | 0.4362 mL | 2.1812 mL | 4.3624 mL |
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2.
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