| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
As a chemical reagent for oligonucleotide synthesis, DMTr-LNA-U-3-CED-Phosphora does not have a defined biological target. Its purpose is to serve as a building block for incorporating LNA uracil residues into synthetic oligonucleotides. LNA modifications significantly enhance the binding affinity and nuclease resistance of oligonucleotides, making this monomer valuable for therapeutic nucleic acid development and molecular biology applications.
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|---|---|
| ln Vitro |
In cell-free biochemical systems, this phosphoramidite monomer is incorporated into oligonucleotide sequences during solid-phase synthesis. The resulting modified oligonucleotides containing LNA uracil residues exhibit dramatically enhanced thermal stability and binding affinity to complementary nucleic acid sequences, with increases of 2-8°C per LNA modification in melting temperature. These properties make LNA-modified oligonucleotides highly effective for antisense, siRNA, and diagnostic applications.
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| ln Vivo |
This compound does not exhibit direct cellular activity as it is a chemical synthesis reagent rather than a bioactive molecule. Oligonucleotides synthesized using this monomer can be delivered into cells for various functional studies. LNA modifications enhance the metabolic stability and binding affinity of oligonucleotides in cellular environments. LNA-modified antisense oligonucleotides and siRNAs show improved potency and duration of action in cells. Cellular uptake typically requires transfection reagents.
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| Enzyme Assay |
The standard procedure for incorporating this phosphoramidite involves solid-phase oligonucleotide synthesis using standard phosphoramidite chemistry. The monomer is dissolved in anhydrous acetonitrile at 0.1 M concentration and coupled to the growing oligonucleotide chain using activator solutions. Coupling times for LNA phosphoramidites are typically extended to 5-10 minutes to ensure efficient incorporation. Following chain assembly, the oligonucleotide is deprotected using ammonium hydroxide treatment.
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| Cell Assay |
No cell-based experimental protocols are directly applicable to this phosphoramidite monomer as it is a chemical synthesis reagent. Oligonucleotides containing LNA uracil residues synthesized using this monomer can be evaluated in cell culture experiments. Typical protocols include transfection of LNA-modified oligonucleotides into mammalian cell lines at concentrations of 1-50 nM. Cells are incubated for 24-72 hours, and target gene knockdown is assessed by qRT-PCR or Western blotting. LNA-modified oligonucleotides often show enhanced potency compared to unmodified oligonucleotides.
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| Animal Protocol |
DMTr-LNA-U-3-CED-Phosphora is not administered to animals as it is a chemical intermediate for oligonucleotide synthesis. Oligonucleotides containing LNA uracil residues synthesized using this monomer may be evaluated in animal models for therapeutic applications. Typical studies involve administration of LNA-modified oligonucleotides to mice or rats via intravenous or subcutaneous routes at doses of 0.5-20 mg/kg. LNA modifications enhance the pharmacokinetic properties and duration of action of oligonucleotides in vivo.
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| ADME/Pharmacokinetics |
As a chemical reagent, this compound does not have established pharmacokinetic properties. Oligonucleotides containing LNA modifications exhibit significantly enhanced metabolic stability and binding affinity compared to unmodified oligonucleotides. LNA modifications increase resistance to nuclease degradation, resulting in prolonged plasma half-lives. Biodistribution is predominantly to liver, kidney, and spleen. The high binding affinity of LNA allows for potent activity at lower doses.
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| Toxicity/Toxicokinetics |
The compound is not intended for therapeutic use and lacks established toxicity profiles. Standard laboratory safety precautions should be observed when handling this chemical reagent. LNA-modified oligonucleotides generally exhibit favorable safety profiles with reduced off-target effects due to their high specificity. However, potential toxicities include hepatotoxicity and immune stimulation at high doses. The maximum tolerated dose depends on the specific oligonucleotide sequence.
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| Additional Infomation |
DMTr-LNA-U-3-CED-Phosphora is a research-grade chemical supplied for oligonucleotide synthesis applications. It is not an approved pharmaceutical and has no clinical trial history as a standalone compound. LNA technology is widely used in therapeutic oligonucleotide development, with multiple LNA-based drugs in clinical development. The compound is typically stored at -20°C under desiccated conditions. Purity specifications generally exceed 98%. This product is for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C40H47N4O9P
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|---|---|
| Molecular Weight |
758.796351671219
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| Exact Mass |
758.31
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| CAS # |
206055-76-7
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| PubChem CID |
23567785
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| Appearance |
White to off-white solid powder
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| LogP |
4.4
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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 |
54
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| Complexity |
1310
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| Defined Atom Stereocenter Count |
4
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| SMILES |
P(N(C(C)C)C(C)C)(OCCC#N)OC1[C@@H]2[C@H](N3C=CC(NC3=O)=O)O[C@@]1(COC(C1C=CC=CC=1)(C1C=CC(=CC=1)OC)C1C=CC(=CC=1)OC)CO2
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| InChi Key |
ROCIJWWVBQZMMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C40H47N4O9P/c1-27(2)44(28(3)4)54(51-24-10-22-41)53-36-35-37(43-23-21-34(45)42-38(43)46)52-39(36,25-49-35)26-50-40(29-11-8-7-9-12-29,30-13-17-32(47-5)18-14-30)31-15-19-33(48-6)20-16-31/h7-9,11-21,23,27-28,35-37H,10,24-26H2,1-6H3,(H,42,45,46)
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| Chemical Name |
3-[[1-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-3-(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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| Synonyms |
DMTr-LNA-U-3-CED-Phosphora
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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: 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) |
DMSO : ~50 mg/mL (~65.9 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.29 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 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 (3.29 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 | 1.3179 mL | 6.5894 mL | 13.1787 mL | |
| 5 mM | 0.2636 mL | 1.3179 mL | 2.6357 mL | |
| 10 mM | 0.1318 mL | 0.6589 mL | 1.3179 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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