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Purity: ≥98%
Azvudine (formerly known as FNC; RO-0622; RO0622) is a novel and potent nucleoside reverse transcriptase inhibitor (NRTI) that has been approved in 2021 in China for the treatment of HIV infection. Azvudine also has the potential to be used for the treatment of novel coronavirus pneumonia (COVID-19). On July 25, 2022, Azvudine was conditionally approved by the Chinese FDA for the treatment of COVID-19, making it the first oral anti-COVID drug in China. RO-0622 and RO-9187 were excellent substrates for deoxycytidine kinase and were phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. As compared with previous reports on ribonucleosides, higher levels of triphosphate were formed from RO-9187 in primary human hepatocytes, and both compounds were potent inhibitors of HCV virus replication in the replicon system (IC(50) = 171 +/- 12 nM and 24 +/- 3 nM for RO-9187 and RO-0622, respectively; CC(50) >1 mM for both). Both compounds inhibited RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations with similar potencies, suggesting no cross-resistance with either R1479 (4'-azidocytidine) or 2'-C-methyl nucleosides. Pharmacokinetic studies with RO-9187 in rats and dogs showed that plasma concentrations exceeding HCV replicon IC(50) values 8-150-fold could be achieved by low dose (10 mg/kg) oral administration. Therefore, 2'-alpha-deoxy-4'-azido nucleosides are a new class of antiviral nucleosides with promising preclinical properties as potential medicines for the treatment of HCV infection.
| Targets |
HIV-1(EC50=0.03-6.92 nM);HIV-2(EC50=0.018-0.02 nM)
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| ln Vitro |
Azvudine (RO-0622) exhibits robust suppression against HIV-1IIIB and HIV-1RF wild-type, with an EC50 varying between 30 and 110 pM. Azvudine has EC50 values of 6.92, 0.34, and 0.45 nM against HIV-1KM018, HIV-1TC-1, and HIV-1WAN T69N, respectively. The PIs-resistant strains HIV-1L10R/M46I/L63P/V82T/I84V and HIV-1RF V82F/184V, the FIs-resistant strain pNL4-3 gp41 (36G) V38A/N42T, and the NRTIs-resistant strain HIV-174V are all susceptible to azvudine. Azvudine's EC50 values against these resistant strains are, in turn, 0.11, 0.14, 0.37, and 0.36 nM[1].
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| References |
| Molecular Formula |
C9H11FN6O4
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|---|---|
| Molecular Weight |
286.2198
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| Exact Mass |
286.08
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| Elemental Analysis |
C, 37.77; H, 3.87; F, 6.64; N, 29.36; O, 22.36
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| CAS # |
1011529-10-4
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| Related CAS # |
Azvudine hydrochloride;1333126-31-0;Azvudine-13C,15N2,d2
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| Appearance |
Solid powder
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| SMILES |
F[C@]1([H])[C@]([H])(N2C(N=C(C([H])=C2[H])N([H])[H])=O)O[C@](C([H])([H])O[H])([C@@]1([H])O[H])N=[N+]=[N-]
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| InChi Key |
KTOLOIKYVCHRJW-XZMZPDFPSA-N
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| InChi Code |
InChI=1S/C9H11FN6O4/c10-5-6(18)9(3-17,14-15-12)20-7(5)16-2-1-4(11)13-8(16)19/h1-2,5-7,17-18H,3H2,(H2,11,13,19)/t5-,6-,7+,9+/m0/s1
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| Chemical Name |
4-amino-1-((2R,3S,4R,5R)-5-azido-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one
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| Synonyms |
Azvudine; FNC; RO-0622; RO 0622; RO0622
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 57~125 mg/mL ( 199.14~436.73 mM )
Water : ~57 mg/mL Ethanol : ~57 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4938 mL | 17.4691 mL | 34.9382 mL | |
| 5 mM | 0.6988 mL | 3.4938 mL | 6.9876 mL | |
| 10 mM | 0.3494 mL | 1.7469 mL | 3.4938 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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