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| Other Sizes |
| Targets |
The primary targets of 2'-O-(2-Methoxyethyl)-cytidine are not traditional biological targets but rather the oligonucleotide sequences into which it is incorporated. As a modified nucleoside, it is used to synthesize oligonucleotides with improved hybridization properties, enhanced stability against nuclease degradation, and reduced immunogenicity. The compound itself does not have direct enzymatic or receptor targets but serves as a building block for therapeutic oligonucleotides.
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| ln Vitro |
In vitro, 2'-O-(2-Methoxyethyl)-cytidine demonstrates good hybridization properties and high stability when incorporated into oligonucleotides. It can be converted from uridine and used in the synthesis of oligonucleotide chemotherapeutic agents. The 2'-O-(2-methoxyethyl) modification enhances the binding affinity of oligonucleotides to complementary RNA or DNA targets and increases resistance to nuclease degradation. The compound itself does not exhibit direct cellular activity but enables the bioactivity of the modified oligonucleotide.
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| ln Vivo |
In vivo activity of 2'-O-(2-Methoxyethyl)-cytidine is associated with the oligonucleotide therapeutics in which it is incorporated. The 2'-O-(2-methoxyethyl) modification improves the pharmacokinetic properties of oligonucleotides, including increased stability in circulation and enhanced tissue distribution. Oligonucleotides containing this modified nucleoside have potential for chemotherapeutic applications. The in vivo efficacy depends on the specific oligonucleotide sequence and target.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not directly applicable for 2'-O-(2-Methoxyethyl)-cytidine, as it is a modified nucleoside building block rather than a bioactive compound. Quality control assays for this compound typically involve HPLC analysis to verify purity (≥98%) and identity. NMR spectroscopy and mass spectrometry are used to confirm the chemical structure. The compound is also tested for its incorporation efficiency into oligonucleotides during synthesis.
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| Cell Assay |
In vitro cellular assays for 2'-O-(2-Methoxyethyl)-cytidine involve testing the complete oligonucleotide in which it is incorporated rather than the nucleoside alone. Cells are treated with the modified oligonucleotide, and effects on target gene expression are measured by qRT-PCR or Western blot. Cell viability and proliferation assays are used to assess the therapeutic potential of the oligonucleotide. The nucleoside itself does not directly affect cell viability but is essential for the function of the modified oligonucleotide.
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| Animal Protocol |
In vivo animal studies for 2'-O-(2-Methoxyethyl)-cytidine are conducted using the final oligonucleotide therapeutic. Animal models of disease are treated with the modified oligonucleotide via various routes of administration. Pharmacokinetic parameters such as half-life, tissue distribution, and clearance are measured. Efficacy is assessed by measuring target gene knockdown and disease progression. The modified nucleoside contributes to the overall stability and PK profile of the oligonucleotide.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 2'-O-(2-Methoxyethyl)-cytidine are determined by the oligonucleotide in which it is incorporated. The compound has a molecular weight of 301.30 and a molecular formula of C₁₂H₁₉N₃O₆. It appears as a white to off-white solid powder with a purity of ≥98%. The 2'-O-(2-methoxyethyl) modification enhances the stability of oligonucleotides in biological fluids, improving their pharmacokinetic profile.
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| Toxicity/Toxicokinetics |
The toxicity profile of 2'-O-(2-Methoxyethyl)-cytidine is associated with the oligonucleotide in which it is used. The compound itself is a modified nucleoside with low intrinsic toxicity. Standard toxicity studies for the final oligonucleotide include assessment of body weight changes, clinical observations, hematological parameters, and histopathological examination of major organs in animal models. The modified nucleoside is generally well-tolerated in research applications.
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| References | |
| Additional Infomation |
2'-O-(2-Methoxyethyl)-cytidine (CAS 223777-16-0) has a molecular formula of C₁₂H₁₉N₃O₆ and a molecular weight of 301.30. The compound appears as a white to off-white solid powder with a purity of ≥98%. It is a synthetic oligonucleotide converted from uridine and is used in the development of chemotherapeutic agents. The 2'-O-(2-methoxyethyl) modification provides good hybridization properties and high stability for oligonucleotide therapeutics. It is intended for research use only and is not approved for clinical use.
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| Molecular Formula |
C12H19N3O6
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|---|---|
| Molecular Weight |
301.30
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| Exact Mass |
301.127
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| CAS # |
223777-16-0
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| PubChem CID |
11077469
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
535.3±60.0 °C at 760 mmHg
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| Flash Point |
277.5±32.9 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
-1.45
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
21
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| Complexity |
441
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
COCCO[C@@H]1[C@@H]([C@H](O[C@H]1N2C=CC(=NC2=O)N)CO)O
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| InChi Key |
YKOGMMXZKKVMBT-QCNRFFRDSA-N
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| InChi Code |
InChI=1S/C12H19N3O6/c1-19-4-5-20-10-9(17)7(6-16)21-11(10)15-3-2-8(13)14-12(15)18/h2-3,7,9-11,16-17H,4-6H2,1H3,(H2,13,14,18)/t7-,9-,10-,11-/m1/s1
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| Chemical Name |
4-amino-1-[(2R,3R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-3-(2-methoxyethoxy)oxolan-2-yl]pyrimidin-2-one
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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 : 250 mg/mL (829.74 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 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: ≥ 2.08 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3190 mL | 16.5948 mL | 33.1895 mL | |
| 5 mM | 0.6638 mL | 3.3190 mL | 6.6379 mL | |
| 10 mM | 0.3319 mL | 1.6595 mL | 3.3190 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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