Osalmid是一种利胆药物，通过靶向核糖核苷酸还原酶小亚基 M2 来抑制核糖核苷酸还原酶的活性，IC50值为8.23 μM。

Osalmid is a choleretic drug, inhibits ribonucleotide reductase activity by targeting ribonucleotide reductase small subunit M2 (RRM2).

Osalmid is identified as a potential ribonucleotide reductase small subunit M2 (RRM2) compound. Osalmid is 10-fold more active in inhibiting ribonucleotide reductase (RR) activity than hydroxyurea, and significantly inhibits HBV DNA and cccDNA synthesis in HepG2.2.15 cells in a time- and dose-dependent manner. The EC50 for HBV DNA inhibition are 11.1 μM for culture supernatant and 16.5 μM for cells after treatment for 8 days with Osalmid. Osalmid suppresses RR activity in a concentration-dependent manner, with an IC50 of 8.23 μM. Osalmid is shown to possess potent activity against a 3TC-resistant HBV strain, suggesting utility in treating drug-resistant HBV infections[1].

Osalmid reduces RR activity and HBV replication in HBV-transgenic mice and exhibits a synergistic efficacy with 3TC without significant toxicity. Oral dosing of osalmid at 400 mg/kg/d causes a time-dependent inhibition of HBV DNA replication. After treatment for 4 weeks, osalmid suppresses HBV DNA replication by about 40-45% as compared to the control in mouse sera and liver tissues[1].

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].

526-18-1

C13H11NO3

229.235

羟苯水杨胺;4'-Hydroxysalicylanilide;Oxaphenamide;柳胺酚

Ethanol:41 mg/mL(178.9 mM)
DMSO:28 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years