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Osalmid

CAS No. : 526-18-1

MCE 站：Osalmid

产品活性：Osalmid是核糖核苷酸还原酶小亚基M2（RRM2）的靶向化合物；抑制核糖核苷酸还原酶活性的IC₅₀值为8.23 μM。

研究领域：Anti-infection

作用靶点：HBV

In Vitro: 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. After treatment for 8 days with Osalmid, the EC₅₀ for HBV DNA inhibition are 11.1 μM for culture supernatant and 16.5 μM for cells. 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.

In Vivo: Osalmid reduces RR activity and HBV replication in HBV-transgenic mice and shows a synergistic efficacy with 3TC without significant toxicity. Oral dosing of osalmid at 400 mg/kg/d results in 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.

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