2-Hydroxy-N-(4-hydroxyphenyl)-benzamide

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Chemical Structure| 526-18-1 同义名 : 羟苯水杨胺 ;4'-Hydroxysalicylanilide;Oxaphenamide;Saryuurin;PHPS;Salmidochol;NSC 93960;Oksafenamid;Auxobil;Osalmid
CAS号 : 526-18-1
货号 : A193150
分子式 : C13H11NO3
纯度 : 98%
分子量 : 229.231
MDL号 : MFCD00020026
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(458.05 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Human ribonucleotide reductase (RR) is the rate-limiting enzyme for DNA synthesis in cells by conversion of ribonucleoside diphosphates (NDPs) to deoxyribonucleoside diphosphates (dNDPs). RRM2 and RRM2B are the regulatory subunits containing a diferric-tyrosyl radical cofactor that is essential for enzyme activity. Osalmid, an approved choleretic drug, is a potential RRM2-targeting inhibitor with an IC50 value of 8.23 μM. In HepG2.2.15 cells, osalmid suppressed the cellular RR activity in a time- and dose-dependent manner. The IC50 in HepG2.2.15 cell lysates was 760.8 μM for osalmid. In HBV DNA-integrated HepG2.2.15 liver cancer cells, osalmid significantly inhibited HBV DNA replication in a time- and dose-dependent manne. Furthermore, osalmid promoted a dose-dependent inhibition of HBV cccDNA levels, suggesting that it can inhibit the synthesis of both HBV genomic DNA and viral cccDNA in infected liver cells. The EC50 for HBV DNA inhibition were 11.1 μM for culture supernatant and 16.5 μM for cells. In HBV-transgenic mice, oral dosing of osalmid at 400 mg/kg/d resulted in a time-dependent inhibition of HBV DNA replication. After treatment for 4 weeks, osalmid suppressed HBV DNA replication by about 40-45% as compared to the control in mouse sera and liver tissues[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.36mL

0.87mL

0.44mL

21.81mL

4.36mL

2.18mL

43.62mL

8.72mL

4.36mL
参考文献

[1]Liu X, Xu Z, et al. Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochem Pharmacol. 2016 Mar 1;103:118-28.

[2]Sadanaga T, Hikida K, et al. Determination of osalmid in plasma by high-performance liquid chromatography. J Chromatogr. 1981 Apr 10;223(1):243-6.

[3]Liu X, Xu Z, Hou C, Wang M, Chen X, Lin Q, Song R, Lou M, Zhu L, Qiu Y, Chen Z, Yang C, Zhu W, Shao J. Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochem Pharmacol. 2016 Mar 1;103:118-28