| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
DMTr-LNA-5MeU-3-CED-phosphoramidite does not have a specific biological target as a drug; rather, it is a synthetic building block used in oligonucleotide synthesis. When incorporated into oligonucleotides, the LNA modification enhances the stability and binding affinity of the oligonucleotide to complementary RNA or DNA sequences. LNA oligonucleotides have improved thermal stability (higher Tm), increased nuclease resistance, and enhanced target specificity. These properties make LNA-modified oligonucleotides valuable tools for antisense therapy, siRNA, miRNA inhibition, and diagnostic applications. The compound's primary function is to serve as a monomer for the synthesis of LNA-containing oligonucleotides.
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| ln Vitro |
In vitro studies of DMTr-LNA-5MeU-3-CED-phosphoramidite focus on its use as a building block for oligonucleotide synthesis rather than as a pharmacologically active compound. The compound is used in solid-phase oligonucleotide synthesis to introduce LNA modifications into oligonucleotides. LNA-modified oligonucleotides exhibit enhanced binding affinity to complementary RNA and DNA, increased nuclease resistance, and improved target specificity. These properties are assessed by measuring melting temperatures (Tm), nuclease stability assays, and binding affinity studies. The compound's purity and stability are assessed by HPLC and mass spectrometry.
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| ln Vivo |
In vivo studies of DMTr-LNA-5MeU-3-CED-phosphoramidite are conducted in the context of LNA-modified oligonucleotides rather than the building block itself. LNA-modified oligonucleotides have been evaluated in various animal models for their therapeutic potential in antisense therapy, siRNA, and other nucleic acid-based therapies. The modifications enhance the stability and efficacy of the oligonucleotides in vivo. In vivo protocols typically involve administration of LNA-modified oligonucleotides via intravenous, subcutaneous, or intraperitoneal injection. Pharmacodynamic endpoints include assessment of target gene knockdown, protein expression, and therapeutic efficacy.
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| Enzyme Assay |
For oligonucleotide synthesis, DMTr-LNA-5MeU-3-CED-phosphoramidite is used in solid-phase synthesis using standard phosphoramidite chemistry. The compound is dissolved in anhydrous acetonitrile and coupled to the growing oligonucleotide chain on a solid support (e.g., controlled pore glass). The coupling reaction is performed in the presence of an activator (e.g., tetrazole or 5-ethylthiotetrazole). After coupling, the phosphite triester is oxidized to phosphate using iodine or other oxidizing agents. The DMTr group is removed by treatment with acid (e.g., trichloroacetic acid) to allow further chain elongation. After synthesis, the oligonucleotide is cleaved from the support and deprotected. The final product is purified by HPLC or PAGE and characterized by mass spectrometry.
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| Cell Assay |
For cellular studies, LNA-modified oligonucleotides synthesized using DMTr-LNA-5MeU-3-CED-phosphoramidite are used to study gene expression and function. Cells are cultured in appropriate medium and transfected with LNA-modified oligonucleotides using lipofection or other transfection methods. Target gene expression is assessed by qRT-PCR and Western blot. Cellular uptake, intracellular localization, and biological activity are evaluated. The LNA modifications enhance the stability and potency of the oligonucleotides in cellular assays.
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| Animal Protocol |
For in vivo studies, LNA-modified oligonucleotides are administered to animals via intravenous, subcutaneous, or intraperitoneal injection. Tissue distribution, pharmacokinetics, and pharmacodynamics are assessed. Target gene knockdown is measured in various tissues by qRT-PCR and Western blot. Therapeutic efficacy is evaluated in disease models. The LNA modifications enhance the stability and bioavailability of the oligonucleotides in vivo.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for DMTr-LNA-5MeU-3-CED-phosphoramidite are not applicable, as the compound is a building block used in oligonucleotide synthesis rather than a therapeutic agent. The pharmacokinetic properties of LNA-modified oligonucleotides depend on the sequence, length, and modification pattern of the oligonucleotide, rather than the building block itself. LNA modifications generally enhance the stability and bioavailability of oligonucleotides in vivo.
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| Toxicity/Toxicokinetics |
Toxicological data for DMTr-LNA-5MeU-3-CED-phosphoramidite are limited, as the compound is a research reagent used in oligonucleotide synthesis. The compound is generally considered to have low toxicity at the concentrations used for synthesis. No acute toxicity, mutagenicity, or carcinogenicity data have been reported. As with all chemical reagents, appropriate safety precautions should be taken when handling DMTr-LNA-5MeU-3-CED-phosphoramidite, including the use of personal protective equipment and work in a well-ventilated area.
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| References | |
| Additional Infomation |
DMTr-LNA-5MeU-3-CED-phosphoramidite (CAS 206055-75-6) is a nucleoside building block used in the synthesis of oligonucleotide-lipid conjugates. It is a modified building block used to enhance stability and binding affinity. The compound has a molecular formula of C₄₁H₄₉N₄O₉P and a molecular weight of 772.82. It contains a 5-methyluridine base, a DMTr protecting group, and a CED phosphoramidite group. LNA-modified oligonucleotides have enhanced stability, nuclease resistance, and target specificity. The compound is strictly for research use only.
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| Molecular Formula |
C41H49N4O9P
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|---|---|
| Molecular Weight |
772.823
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| Exact Mass |
772.323
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| CAS # |
206055-75-6
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| PubChem CID |
11343250
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| Appearance |
White to off-white solid powder
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
55
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| Complexity |
1350
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)N(C(C)C)P(OCCC#N)O[C@@H]([C@@H](OC1)[C@H](N2C(NC(C(C)=C2)=O)=O)O3)[C@@]31COC(C4=CC=C(OC)C=C4)(C5=CC=CC=C5)C6=CC=C(OC)C=C6
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| InChi Key |
STPXOEPMLLHUDQ-ZRCIEBSPSA-N
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| InChi Code |
InChI=1S/C41H49N4O9P/c1-27(2)45(28(3)4)55(52-23-11-22-42)54-36-35-38(44-24-29(5)37(46)43-39(44)47)53-40(36,25-50-35)26-51-41(30-12-9-8-10-13-30,31-14-18-33(48-6)19-15-31)32-16-20-34(49-7)21-17-32/h8-10,12-21,24,27-28,35-36,38H,11,23,25-26H2,1-7H3,(H,43,46,47)/t35-,36+,38-,40-,55?/m1/s1
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| Chemical Name |
3-[[(1R,3R,4R,7S)-1-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-3-(5-methyl-2,4-dioxopyrimidin-1-yl)-2,5-dioxabicyclo[2.2.1]heptan-7-yl]oxy-[di(propan-2-yl)amino]phosphanyl]oxypropanenitrile
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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 (~323.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.69 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 (2.69 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 20.8 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 | 1.2940 mL | 6.4698 mL | 12.9396 mL | |
| 5 mM | 0.2588 mL | 1.2940 mL | 2.5879 mL | |
| 10 mM | 0.1294 mL | 0.6470 mL | 1.2940 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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