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Fomivirsen sodium is a novel and potent antisense 21 mer phosphorothioate oligonucleotide with antiviral activity. As an antiviral agent, it can be used for cytomegalovirus retinitis (CMV). Fomivirsen sodium acts by binding to and degrading the mRNAs encoding CMV immediate-early 2 protein (required for viral replication), thus providing bioactive effects for CMV retinitis by inhibition of virus proliferation.
| ln Vitro |
Via the antisense mechanism, antisense oligonucleotides impede viral replication by complementing the messenger RNA of the main early region protein of the human cytomegalovirus [1]. The 21-mer phosphorothioate ASO Fomiwesen sodium has a CpG motif close to its 5' terminator. Its sequence, 5'-GCG TTT GCT CTT CTT CTT GCG-3', results in mRNA regulation by an RNase H-mediated mechanism[2]. Human fibroblasts (MRC-5 cells) and pigment epithelial (RPE) cells' CMV replication is dose-regulated by fomiwesen sodium. RPE cells have an average IC50 of 0.03 μM, while MRC5 cells have an average IC50 of 0.2 μM[1].
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| References |
[1]. M D de Smet, et al. Fomivirsen- a phosphorothioate oligonucleotide for the treatment of CMV retinitis. Ocul Immunol Inflamm. 1999 Dec;7(3-4):189-98.
[2]. Anna Kilanowska, et al. In vivo and in vitro studies of antisense oligonucleotides – a review. (Review Article) RSC Adv., 2020, 10, 34501-34516 |
| Molecular Formula |
C204H243N63NA20O114P20S20
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|---|---|
| Molecular Weight |
7122.03656983376
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| CAS # |
160369-77-7
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| Related CAS # |
Fomivirsen;144245-52-3
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| SMILES |
S=P([O-])(OC[C@@H]1[C@H](C[C@H](N2C=NC3C(NC(N)=NC2=3)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(N=C(C=C2)N)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(N=C(C=C2)N)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(N=C(C=C2)N)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(N=C(C=C2)N)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(NC(C(C)=C2)=O)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C=NC3C(NC(N)=NC2=3)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C(N=C(C=C2)N)=O)O1)OP([O-])(OC[C@@H]1[C@H](C[C@H](N2C=NC3C(NC(N)=NC2=3)=O)O1)O)=S)=S)=S)=S)=S)=S)=S)=S)=S)=S)=S)=S)=S)=S)O[C@H]1C[C@H](N2C(NC(C(C)=C2)=O)=O)O[C@@H]1COP([O-])(O[C@H]1C[C@H](N2C(NC(C(C)=C2)=O)=O)O[C@@H]1COP([O-])(O[C@H]1C[C@H](N2C(NC(C(C)=C2)=O)=O)O[C@@H]1COP([O-])(O[C@H]1C[C@H](N2C=NC3C(NC(N)=NC2=3)=O)O[C@@H]1COP([O-])(O[C@H]1C[C@H](N2C(N=C(C=C2)N)=O)O[C@@H]1COP([O-])(O[C@@H]1[C@@H](CO)O[C@H](C1)N1C=NC2C(NC(N)=NC1=2)=O)=S)=S)=S)=S)=S.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~14.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (14.04 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.1404 mL | 0.7020 mL | 1.4041 mL | |
| 5 mM | 0.0281 mL | 0.1404 mL | 0.2808 mL | |
| 10 mM | 0.0140 mL | 0.0702 mL | 0.1404 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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