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Inarigivir

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Chemical Structure| 475650-36-3 同义名 : ORI-9020;SB-9000
CAS号 : 475650-36-3
货号 : A167476
分子式 : C20H26N7O10PS
纯度 : 99%+
分子量 : 587.5
MDL号 : MFCD31727872
存储条件:

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 190 mg/mL(323.4 mM),配合低频超声助溶,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 Chronic hepatitis B virus infection (HBV) continues to pose a serious global health threat in many areas of the world, particularly in sub-Saharan Africa, the Western Pacific Region and areas of Eastern Europe[1]. Inarigivir, a novel dinucleotide, evaluated in transgenic mice expressing HBV, significantly reduced liver HBV DNA (P ≤ 0.001)[2]. The mode of antiviral action of Inarigivir appears to be direct interference of HBV replication at the level of HBV reverse transcriptase and/or DNA polymerase at an early step, either at, or prior to, the production of the first strand of HBV DNA. I.p. injection of Inarigivir at 100 mg/kg/day significantly reduced viral DNA in the liver (P ≤ 0.001) and showed anti-HBV activity similar to that of ADV. The minimal effective dosage of Inarigivir was identified to be between 1.6 and 0.5 mg/kg/day using liver HBV DNA values[2].
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
NCT03493698 Drug Interaction Potentiation Phase 1 Completed - Netherlands ... 展开 >> University Medical Center Groningen Groningen, Netherlands 收起 <<
NCT03434353 Chronic Hepatitis b Phase 2 Recruiting June 2020 Hong Kong ... 展开 >> Alice Ho Miu Ling Nethersole Hospital Recruiting Hong Kong, Hong Kong Prince of Wales Hospital-HK Recruiting Hong Kong, Hong Kong Korea, Republic of Korea University Ansan Hospital Recruiting Ansan, Korea, Republic of, 425-707 Keimyung University Dongsan Medical Center Recruiting Daegu, Korea, Republic of, 41931 Kyungpook National University Hospital Recruiting Daegu, Korea, Republic of, 41944 Inje University Ilsan Paik Hospital Recruiting Ilsan, Korea, Republic of, 10380 Severance Hospital, Yonsei University Health System Recruiting Seoul, Korea, Republic of, 03722 Asan Medical Center Recruiting Seoul, Korea, Republic of, 05505 Gangnam Severance Hospital, Yonsei University Health System Recruiting Seoul, Korea, Republic of, 06273 Catholic University of Korea, Seoul Saint Mary's Hospital Recruiting Seoul, Korea, Republic of, 06591 SMG-SNU Boramae Medical Center Recruiting Seoul, Korea, Republic of, 07061 Korea University Guro Hospital Recruiting Seoul, Korea, Republic of, 08308 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.51mL

1.70mL

0.85mL

17.02mL

3.40mL

1.70mL

参考文献

[1]Ginzberg D, Wong RJ, Gish R. Global HBV burden: guesstimates and facts. Hepatol Int. 2018 Jul;12(4):315-329. doi: 10.1007/s12072-018-9884-8. Epub 2018 Jul 27. PMID: 30054801.

[2]Iyer RP, Roland A, Jin Y, Mounir S, Korba B, Julander JG, Morrey JD. Anti-hepatitis B virus activity of ORI-9020, a novel phosphorothioate dinucleotide, in a transgenic mouse model. Antimicrob Agents Chemother. 2004 Jun;48(6):2318-20. doi: 10.1128/AAC.48.6.2318-2320.2004. PMID: 15155244; PMCID: PMC415565.