Azvudine hydrochloride
(Synonyms: RO-0622 hydrochloride; FNC hydrochloride) 目录号 : GC60071
Azvudine hydrochloride 是一种有效的核苷逆转录酶抑制剂 (NRTI)，对 HIV、HBV 和 HCV（HIV-1（EC50 0.03 至 6.92 nM）和 HIV-2（EC50 0.018 至 0.025 nM））具有抗病毒活性。
Cas No.:1333126-31-0
Sample solution is provided at 25 µL, 10mM.
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Azvudine hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI) that has antiviral activity against HIV, HBV, and HCV,(HIV-1 (EC50s 0.03 to 6.92 nM) and HIV-2 (EC50s 0.018 to 0.025 nM))[1]. Azivudine hydrochloride could inhibit SARS-CoV-2 and HCoV-OC43 coronavirus with EC50 1.2-4.3 μM[3].
In C8166 cells,Azvudine hydrochloride showed strong inhibition against wild-type HIV-1 IIIB and HIV-1 RF, with 50% effective concentration values (EC 50) ranging from 30 to 110 pM[2].
EV71 and CA16 challenge resulted in 90% and 30% mortality, respectively, while Azvudine hydrochloride treatment greatly reduced mortality to 20% and 0%. Azvudine hydrochloride treatment significantly improved clinical presentation and survival, indicating that Azvudine hydrochloride effectively protects against EV71 and CA16 challenge in vivo[4].
Treating SARS-CoV-2 infected rhesus macaques with Azvudine hydrochloride (0.07 mg/kg, qd, orally) reduced viral load, recuperated the thymus, improved lymphocyte profiles, alleviated inflammation and organ damage, and lessened ground-glass opacities in chest X-ray[3].
Azvudine hydrochloride clinical efficacy in curing COVID-19 was significant, showing inhibition of SARS-CoV-2 replication in all 31 patients after treatment with Azvudine hydrochloride, and the anti-coronavirus activity of Azvudine hydrochloride was also demonstrated in animal experiments using RM[5].
References:
[1]: Wang RR, Yang QH, et,al. Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in vitro. PLoS One. 2014 Aug 21;9(8):e105617. doi: 10.1371/journal.pone.0105617. PMID: 25144636; PMCID: PMC4140803.
[2]: Zhou Y, Zhang Y, et,al.Novel nucleoside analogue FNC is effective against both wild-type and lamivudine-resistant HBV clinical isolates. Antivir Ther. 2012;17(8):1593-9. doi: 10.3851/IMP2292. Epub 2012 Aug 9. PMID: 22910281.
[3]: Zhang JL, Li YH, et,al. Azvudine is a thymus-homing anti-SARS-CoV-2 drug effective in treating COVID-19 patients. Signal Transduct Target Ther. 2021 Dec 6;6(1):414. doi: 10.1038/s41392-021-00835-6. PMID: 34873151; PMCID: PMC8646019.
[4]: Xu N, Yang J, et,al.The Pyrimidine Analog FNC Potently Inhibits the Replication of Multiple Enteroviruses. J Virol. 2020 Apr 16;94(9):e00204-20. doi: 10.1128/JVI.00204-20. PMID: 32075935; PMCID: PMC7163137.
[5]: Ren Z, Luo H, et,al. A Randomized, Open-Label, Controlled Clinical Trial of Azvudine Tablets in the Treatment of Mild and Common COVID-19, a Pilot Study. Adv Sci (Weinh). 2020 Aug 13;7(19):2001435. doi: 10.1002/advs.202001435. PMID: 32837847; PMCID: PMC7404576.
[6]: Fayzullina D, Kharwar RK, et,al. FNC: An Advanced Anticancer Therapeutic or Just an Underdog? Front Oncol. 2022 Feb 10;12:820647. doi: 10.3389/fonc.2022.820647. PMID: 35223502; PMCID: PMC8867032.
Azvudine hydrochloride 是一种有效的核苷逆转录酶抑制剂 (NRTI)，对 HIV、HBV 和 HCV（HIV-1（EC50 0.03 至 6.92 nM）和 HIV-2（EC50 0.018 至 0.025 nM））具有抗病毒活性[1]。盐酸阿齐夫定对SARS-CoV-2和HCoV-OC43冠状病毒具有抑制作用，EC50为1.2-4.3 μM[3]。
在 C8166 细胞中，盐酸阿兹夫定对野生型 HIV-1 IIIB 和 HIV-1 RF 表现出强烈的抑制作用，50% 有效浓度值 (EC 50) 范围为 30 至 110 pM[2].
EV71 和 CA16 攻击分别导致 90% 和 30% 的死亡率，而盐酸阿兹夫定处理将死亡率大大降低至 20% 和 0%。阿兹夫定盐酸盐治疗显着改善了临床表现和生存率，表明阿兹夫定盐酸盐可有效保护体内免受 EV71 和 CA16 攻击[4]。
用盐酸阿兹夫定（0.07 毫克/千克，每日一次，口服）治疗感染 SARS-CoV-2 的恒河猴，可降低病毒载量，恢复胸腺，改善淋巴细胞分布，减轻炎症和器官损伤，并减轻毛玻璃样混浊胸部 X 光片[3].
盐酸阿兹夫定治疗 COVID-19 的临床疗效显着，在所有 31 名接受盐酸阿兹夫定治疗后的患者中均表现出抑制 SARS-CoV-2 复制的作用，并且在动物实验中也证明了盐酸阿兹夫定的抗冠状病毒活性RM[5].
| Cell experiment [1]: | |
|
Cell lines |
C8166 cells |
|
Preparation Method |
Cells were seeded each well in a 96-well plate with Azvudine hydrochloride . The plate was placed in a humidified incubator. After incubation of 3-7 days, the percentage inhibition of syncytia formation was scored or the level of p24 was measured by ELISA and 50% effective concentration (EC50) were calculated. |
|
Reaction Conditions |
2nM Azvudine hydrochloride for 3-7 days at 37°C |
|
Applications |
Azvudine hydrochloride showed strong inhibition against wild-type HIV-1 IIIB and HIV-1 RF, with 50% effective concentration values (EC 50) ranging from 30 to 110 pM. |
| Animal experiment [2]: | |
|
Animal models |
Lethal EV71 and CA16 infection in neonatal mouse models |
|
Preparation Method |
The neonatal mice were randomly divided into five groups, and each group contained three litters . One group was inoculated intracerebrally with DMEM (10 µl/mouse) and after 1 h injected intraperitoneally with DMSO. Two groups were inoculated intracerebrally with EV71 CC063 and after 1 h injected intraperitoneally with Azvudine hydrochloride or DMSO. Azvudine hydrochloride was injected intraperitoneally on days 1, 3, 6, 9, and 12 |
|
Dosage form |
1 mg/kg Azvudine hydrochloride on days 1, 3, 6, 9, and 12 |
|
Applications |
EV71 and CA16 challenge resulted in 90% and 30% mortality, respectively, while Azvudine hydrochloride Azvudine hydrochloride treatment greatly reduced mortality to 20% and 0%. Azvudine hydrochloride treatment significantly improved clinical presentation and survival, indicating that FNC effectively protects against EV71 and CA16 challenge in vivo. |
|
References: [1]. Wang RR, Yang QH,et,al. Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in vitro. PLoS One. 2014 Aug 21;9(8):e105617. doi: 10.1371/journal.pone.0105617. PMID: 25144636; PMCID: PMC4140803. | |
| Cas No. | 1333126-31-0 | SDF | |
| 别名 | RO-0622 hydrochloride; FNC hydrochloride | ||
| Canonical SMILES | NC(C=CN1[C@@H]2O[C@@](N=[N+]=[N-])([C@H]([C@@H]2F)O)CO)=NC1=O.[H]Cl | ||
| 分子式 | C9H12ClFN6O4 | 分子量 | 322.68 |
| 溶解度 | Water: 125 mg/mL (387.38 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.099 mL | 15.4952 mL | 30.9905 mL |
| 5 mM | 0.6198 mL | 3.099 mL | 6.1981 mL |
| 10 mM | 0.3099 mL | 1.5495 mL | 3.099 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet