Catalog Number
ACM1011529104
Description
Azvudine, also known as FNC and RO-0622, is a reverse transcriptase inhibitor potentially for the treatment of HIV infection. Azvudine showed synergism in combination with six approved anti-HIV drugs on both C8166 and PBMC. Azvudine also showed potent inhibition on NRTI-resistant strains (L74V and T69N). Treatment with Azudine and the protein biosynthesis inhibitor, cycloheximide (CHX), accelerated the inhibition of viral protein synthesis in the HTLV‑1‑infected cells.
Synonyms
Azvudine; FNC; RO-0622; RO 0622; RO0622
IUPAC Name
4-amino-1-((2R,3S,4R,5R)-5-azido-3-fluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one
Molecular Formula
C9H11FN6O4
Canonical SMILES
O=C1N=C(N)C=CN1[C@H]2[C@@H](F)[C@@H]([C@](CO)(N=[N+]=[N-])O2)O
InChI
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
InChI Key
KTOLOIKYVCHRJW-XZMZPDFPSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV that exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 37.77; H, 3.87; F, 6.64; N, 29.36; O, 22.36
HS Tariff Code
2934.99.9001
In Vitro Activity
To evaluate the antiviral activity of Azvudine (FNC), the lab-adaptive strains (IIIB, RF) and clinical strains (KM018, TC-1, WAN) were used to infect HIV sensitive C8166 cells or PHA-stimulated PBMCs and the commercially available NRTI-3TC was used as control. FNC displayed strong inhibition on wild-type HIV-1IIIB and HIV-1RF with the 50% effective concentration values (EC50) ranging from 30 to 110 pM. FNC was about 1835- to 11671-fold more potent than 3TC. FNC was also inhibitory to HIV-2ROD and HIV-2CBL-20 in vitro with EC50 of 0.018 and 0.025 nM respectively.
Reference: PLoS One. 2014 Aug 21. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4140803/
In Vivo Activity
Oral administration of FNC in rats revealed a substantial thymus-homing feature, with FNC triphosphate (the active form) concentrated in the thymus and peripheral blood mononuclear cells (PBMC). Treating SARS-CoV-2 infected rhesus macaques with FNC (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.
Reference: Signal Transduct Target Ther. 2021 Dec 6. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8646019/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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