| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
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| Other Sizes |
| Targets |
The primary targets of 2'-Deoxy-5'-O-DMT-2'-fluorouridine are not biological, as it is a synthetic intermediate. However, its incorporation into oligonucleotides targets specific mRNA sequences for therapeutic purposes, such as gene silencing. The 2'-fluoro modification enhances the stability and pharmacokinetic properties of the resulting oligonucleotide therapeutics.
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|---|---|
| ln Vitro |
At concentrations up to 20 mM, 2'-Deoxy-5'-O-DMT-2'-fluorouridine (compound 15h) exhibits 100% inhibition against YFV. It also demonstrates noncytotoxicity.
In vitro, this compound is used as a monomer in solid-phase oligonucleotide synthesis. It is not tested for biological activity on its own. The resulting oligonucleotides containing this modified nucleoside have been shown to have increased thermal stability and resistance to nuclease degradation, making them more effective in antisense and RNAi applications. |
| ln Vivo |
In vivo, the compound itself is not administered. However, oligonucleotides synthesized with this building block have been studied in animal models for various diseases, including cancer and viral infections. The 2'-fluoro modification contributes to improved bioavailability and prolonged circulation time of these therapeutic oligonucleotides.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to this compound, as it is a chemical building block. Quality control assays involve HPLC, NMR, and mass spectrometry to verify purity, identity, and correct protecting groups. The compound is tested for solubility and stability in various solvents used in oligonucleotide synthesis.
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| Cell Assay |
In vitro cellular assays are not performed with this building block; they are conducted with the final oligonucleotides. However, the building block's quality is assessed by its coupling efficiency in solid-phase synthesis, which is monitored by trityl yield and HPLC of the final product.
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| Animal Protocol |
In vivo animal studies are not conducted with this compound directly. The final oligonucleotides containing this modified nucleoside are tested in pharmacokinetic and efficacy studies. The building block is not intended for in vivo administration.
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| ADME/Pharmacokinetics |
2'-Deoxy-5'-O-DMT-2'-fluorouridine has a molecular formula of C30H29FN2O7 and a molecular weight of 548.56. It appears as a white to off-white solid powder with a purity of ≥98%. It is soluble in DMSO and dichloromethane. The compound should be stored at -20°C, protected from moisture, and is stable for long periods under dry conditions. It is intended for research use only and is not for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of this building block is not characterized, as it is a chemical intermediate. Standard laboratory safety precautions should be followed. It is not intended for clinical use.
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| References | |
| Additional Infomation |
2'-Deoxy-5'-O-DMT-2'-fluorouridine (CAS 146954-74-7) is a modified nucleoside used as a building block for oligonucleotide synthesis. It has a molecular formula of C30H29FN2O7 and a molecular weight of 548.56. The compound contains a 2'-fluoro modification that enhances nuclease resistance and binding affinity of oligonucleotides, and a 5'-O-DMT protecting group for selective deprotection. It is used in the synthesis of antisense and siRNA therapeutics. It is intended for research use only and is not approved for clinical use.
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| Molecular Formula |
C30H29FN2O7
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|---|---|
| Molecular Weight |
548.56
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| Exact Mass |
548.195
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| CAS # |
146954-74-7
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| PubChem CID |
7073186
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.647
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| LogP |
4.83
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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 |
9
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| Heavy Atom Count |
40
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| Complexity |
873
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| Defined Atom Stereocenter Count |
4
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| SMILES |
COC1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=C(C=C3)OC)OC[C@@H]4[C@H]([C@H]([C@@H](O4)N5C=CC(=O)NC5=O)F)O
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| InChi Key |
CSSFZSSZXOCCJB-YULOIDQLSA-N
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| InChi Code |
InChI=1S/C30H29FN2O7/c1-37-22-12-8-20(9-13-22)30(19-6-4-3-5-7-19,21-10-14-23(38-2)15-11-21)39-18-24-27(35)26(31)28(40-24)33-17-16-25(34)32-29(33)36/h3-17,24,26-28,35H,18H2,1-2H3,(H,32,34,36)/t24-,26-,27-,28-/m1/s1
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| Chemical Name |
1-[(2R,3R,4R,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-3-fluoro-4-hydroxyoxolan-2-yl]pyrimidine-2,4-dione
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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 (182.30 mM)
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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 | 1.8230 mL | 9.1148 mL | 18.2295 mL | |
| 5 mM | 0.3646 mL | 1.8230 mL | 3.6459 mL | |
| 10 mM | 0.1823 mL | 0.9115 mL | 1.8230 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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