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Osalmid(Oxaphenamide)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Osalmid(Oxaphenamide)图片
CAS NO:526-18-1
规格:98%
分子量:229.23
包装与价格:
包装价格(元)
100mg电议
500mg电议
1g电议

产品介绍
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8.23μM。
CAS:526-18-1
分子式:C13H11NO3
分子量:229.23
纯度:98%
存储:Store at -20°C

Background:

Osalmid is a ribonucleotide reductase small subunit M2 (RRM2) targeting compound; suppresses ribonucleotide reductase activity with an IC50 of 8.23 μM.


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[1].


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[1].


[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.