| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
5'-O-DMT-N4-Bz-2'-F-dC does not have a specific biological target itself but serves as a protected and modified nucleoside building block for oligonucleotide therapeutics. When incorporated into oligonucleotides, the 2'-fluoro modification enhances nuclease resistance, increases binding affinity to complementary RNA targets, and reduces immunogenicity. The DMT group provides 5'-hydroxyl protection for controlled chain elongation, while the benzoyl group protects the exocyclic amine of cytosine. The 2'-fluoro modification is commonly used in antisense and siRNA therapeutics.
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|---|---|
| ln Vitro |
In vitro activity of 5'-O-DMT-N4-Bz-2'-F-dC is assessed by its utility as a building block in oligonucleotide synthesis. The efficiency of incorporation into growing oligonucleotide chains during solid-phase synthesis is evaluated by monitoring coupling efficiency. The resulting modified oligonucleotides are evaluated for their binding affinity to complementary RNA targets using thermal melting (Tm) analysis, with the 2'-fluoro modification typically increasing Tm. Nuclease resistance is assessed by incubation with various nucleases followed by gel electrophoresis or HPLC analysis.
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| ln Vivo |
In vivo studies for 5'-O-DMT-N4-Bz-2'-F-dC are typically conducted on the modified oligonucleotides incorporating this nucleoside rather than the protected monomer itself. These oligonucleotides are evaluated in animal models for their pharmacokinetic properties, biodistribution, and therapeutic efficacy in applications such as antisense therapy or siRNA. The 2'-fluoro modification enhances metabolic stability and reduces immunogenicity of therapeutic oligonucleotides, potentially improving their in vivo performance.
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| Enzyme Assay |
For oligonucleotide synthesis, 5'-O-DMT-N4-Bz-2'-F-dC is converted to the corresponding phosphoramidite and incorporated into oligonucleotides using standard solid-phase synthesis protocols. Coupling efficiency is monitored by trityl cation release measurements. After synthesis, the oligonucleotide is cleaved from the solid support and deprotected using appropriate reagents. The 2'-fluoro modification is stable during synthesis and deprotection. The final oligonucleotide is purified by HPLC or PAGE and characterized by mass spectrometry.
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| Cell Assay |
For cellular uptake and activity studies, cultured cells are treated with modified oligonucleotides containing 5'-O-DMT-N4-Bz-2'-F-dC. Cells are incubated with oligonucleotides for 24-72 hours, and cellular uptake is assessed by fluorescence microscopy or flow cytometry using fluorescently labeled oligonucleotides. For antisense applications, gene knockdown efficiency is evaluated by qRT-PCR or Western blot. For siRNA applications, target gene silencing is assessed at the mRNA and protein levels. Cytotoxicity is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
For in vivo evaluation of modified oligonucleotides, mice or rats are administered the oligonucleotides via various routes. Pharmacokinetic parameters including half-life, clearance, and tissue distribution are determined by measuring oligonucleotide concentrations in plasma and tissues using hybridization-based assays or LC-MS. For therapeutic applications, efficacy is evaluated in appropriate disease models (e.g., tumor xenografts for antisense therapy), with tumor volume or disease biomarkers monitored over time. Toxicity is assessed by monitoring body weight, organ histopathology, and serum chemistry.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 5'-O-DMT-N4-Bz-2'-F-dC are typically characterized for the modified oligonucleotides incorporating this nucleoside. The 2'-fluoro modification increases metabolic stability by reducing susceptibility to nuclease degradation. The compound has a molecular weight of 651.68. Detailed PK parameters depend on the specific oligonucleotide sequence, length, and backbone chemistry. The modification may also affect cellular uptake and tissue distribution. Storage at -20°C is recommended.
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| Toxicity/Toxicokinetics |
5'-O-DMT-N4-Bz-2'-F-dC is a research compound intended for laboratory use only and is not approved for human therapeutic use. As a modified nucleoside, it is used in the design of modified DNA and RNA analogs for therapeutic and diagnostic applications. The compound features a 2'-fluoro modification that enhances nuclease resistance. Standard laboratory safety precautions should be followed when handling this compound. Storage at -20°C is recommended.
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| Additional Infomation |
5'-O-DMT-N4-Bz-2'-F-dC is a nucleoside with protective and modifying effects, with molecular formula C37H34FN3O7 and molecular weight 651.68. It features a 2'-fluoro modification that enhances nuclease resistance and binding affinity, used in antisense oligonucleotides, siRNAs, and aptamers. The compound is for research use only and has not been approved for clinical applications. Storage at -20°C is recommended.
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| Molecular Formula |
C37H34FN3O7
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|---|---|
| Molecular Weight |
651.680173397064
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| Exact Mass |
651.238
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| CAS # |
146954-77-0
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| PubChem CID |
10055052
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| Appearance |
White to off-white solid powder
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
48
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
4
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| SMILES |
F[C@H]1[C@H](N2C(N=C(C=C2)NC(C2C=CC=CC=2)=O)=O)O[C@H](COC(C2C=CC=CC=2)(C2C=CC(=CC=2)OC)C2C=CC(=CC=2)OC)[C@H]1O
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| InChi Key |
RAIBEZUVTIPFOJ-NHASGABXSA-N
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| InChi Code |
InChI=1S/C37H34FN3O7/c1-45-28-17-13-26(14-18-28)37(25-11-7-4-8-12-25,27-15-19-29(46-2)20-16-27)47-23-30-33(42)32(38)35(48-30)41-22-21-31(40-36(41)44)39-34(43)24-9-5-3-6-10-24/h3-22,30,32-33,35,42H,23H2,1-2H3,(H,39,40,43,44)/t30-,32-,33-,35-/m1/s1
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| Chemical Name |
N-[1-[(2R,3R,4R,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-3-fluoro-4-hydroxyoxolan-2-yl]-2-oxopyrimidin-4-yl]benzamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : 100 mg/mL (153.45 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.84 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5345 mL | 7.6725 mL | 15.3450 mL | |
| 5 mM | 0.3069 mL | 1.5345 mL | 3.0690 mL | |
| 10 mM | 0.1534 mL | 0.7672 mL | 1.5345 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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