|2-羟基-N-(4-羟基苯基)苯甲酰胺|CsnPharm

CAS No.: 526-18-1

2-Hydroxy-N-(4-hydroxyphenyl)-benzamide/柳胺酚 Catalog No. CSN16749

Synonyms: Oxaphenamide;4'-Hydroxysalicylanilide;Auxobil

Osalmid can target ribonucleotide reductase small subunit M2 (RRM2) with IC50 of 8.23 μM. It is used for cholecystitis and bile duct inflammation.

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实验方案

技术信息

生物活性

靶点 Ribonucleotide Reductase

IC50:8.23μM
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].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT03670173 Multiple Myeloma Phase 1 Phase 2 Not yet recruiting September 30, 2020 -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03670173	Multiple Myeloma	Phase 1 Phase 2	Not yet recruiting	September 30, 2020	-

[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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.3624 mL
- 21.8120 mL
- 43.6241 mL
- 5 mM
- 0.8725 mL
- 4.3624 mL
- 8.7248 mL
- 10 mM
- 0.4362 mL
- 2.1812 mL
- 4.3624 mL

技术信息

CAS号

526-18-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H11NO3

运输

蓝冰

分子量

229.23

别名

Oxaphenamide;4'-Hydroxysalicylanilide;Auxobil;Oksafenamid;NSC-93960;Salmidochol;PHPS;Saryuurin;羟苯水杨胺

溶解度

DMSO	43.0 mg/mL (187.6 mM)
Water	Insoluble
Ethanol	45.0 mg/mL (196.3 mM)

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2-Hydroxy-N-(4-hydroxyphenyl)-benzamide/柳胺酚 Catalog No. CSN16749

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