| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
DMT-dA(PAc) Phosphoramidite does not have a specific biological target itself but serves as a building block for oligonucleotide synthesis. When incorporated into oligonucleotides, the resulting sequences can target various biological molecules including mRNA (for antisense applications), DNA (for PCR and sequencing), or proteins (for aptamer applications). The DMT group provides 5'-hydroxyl protection for controlled chain elongation, while the PAc group protects the exocyclic amine of adenine during synthesis. The compound has been used in the synthesis of cyclic dinucleotide prodrugs as STING agonists.
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| ln Vitro |
In vitro activity of DMT-dA(PAc) Phosphoramidite 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 through trityl cation release measurements. The purity of the compound and its suitability for automated DNA synthesis are assessed by HPLC analysis. The resulting oligonucleotides are evaluated for their ability to hybridize to complementary sequences using thermal melting (Tm) analysis and for their biological activity in various assays depending on the specific application.
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| ln Vivo |
In vivo studies for DMT-dA(PAc) Phosphoramidite are typically conducted on the oligonucleotides synthesized using this building block rather than the phosphoramidite itself. These oligonucleotides are evaluated in animal models for their pharmacokinetic properties, biodistribution, and therapeutic efficacy in applications such as antisense therapy, siRNA, or STING agonist development. The protecting groups (DMT and PAc) are removed during oligonucleotide synthesis and deprotection, so the final oligonucleotide contains the natural deoxyadenosine nucleoside.
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| Enzyme Assay |
For oligonucleotide synthesis, DMT-dA(PAc) Phosphoramidite is dissolved in anhydrous acetonitrile and coupled to the growing oligonucleotide chain using standard solid-phase synthesis protocols. Coupling efficiency is monitored by trityl cation release measurements at each synthesis cycle. After synthesis, the oligonucleotide is cleaved from the solid support and deprotected using ammonium hydroxide or other appropriate reagents. The PAc group is removed under mild conditions, allowing for efficient deprotection. The final oligonucleotide is purified by HPLC or PAGE and characterized by mass spectrometry.
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| Cell Assay |
For cellular studies, cultured cells are treated with oligonucleotides synthesized using DMT-dA(PAc) Phosphoramidite as a building block. 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 STING agonist applications, STING activation is assessed by measuring interferon-β production or STING pathway activation markers. Cytotoxicity is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
For in vivo evaluation of oligonucleotides synthesized using DMT-dA(PAc) Phosphoramidite, 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. For STING agonists, efficacy in cancer models is assessed by tumor growth inhibition and immune activation markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DMT-dA(PAc) Phosphoramidite are characterized for the oligonucleotides incorporating this building block rather than the phosphoramidite itself. The compound has a molecular weight of 887.96 and is typically handled as a solid. The PAc protecting group allows for milder deprotection conditions, which can be beneficial for sensitive oligonucleotide sequences. Detailed PK parameters depend on the specific oligonucleotide sequence, length, and backbone chemistry. Storage at -20°C under inert gas is recommended.
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| Toxicity/Toxicokinetics |
DMT-dA(PAc) Phosphoramidite is a research compound intended for laboratory use only and is not approved for human therapeutic use. As a phosphoramidite building block, it is used in DNA and RNA oligonucleotide synthesis for various research applications. The compound features DMT and PAc protecting groups. Standard laboratory safety precautions should be followed when handling this compound. Storage at -20°C under inert gas is recommended.
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| References | |
| Additional Infomation |
DMT-dA(PAc) Phosphoramidite is a nucleoside phosphoramidite building block with molecular formula C48H54N7O8P and molecular weight 887.96. It is used in solid-phase DNA and RNA synthesis, featuring DMT protection of the 5'-hydroxyl and PAc protection of the adenine exocyclic amine. The compound has been used in the synthesis of cyclic dinucleotide prodrugs as STING agonists. It is for research use only and has not been approved for clinical applications. Storage at -20°C under inert gas is recommended.
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| Molecular Formula |
C48H54N7O8P
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|---|---|
| Molecular Weight |
887.96
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| Exact Mass |
887.377
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| CAS # |
110543-74-3
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| PubChem CID |
13888020
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| Appearance |
White to off-white solid powder
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| LogP |
8.891
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
64
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| Complexity |
1420
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC(C)N(C(C)C)P(OCCC#N)O[C@H]1C[C@@H](O[C@@H]1COC(C2=CC=CC=C2)(C3=CC=C(C=C3)OC)C4=CC=C(C=C4)OC)N5C=NC6=C(N=CN=C65)NC(=O)COC7=CC=CC=C7
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| InChi Key |
INUFZOANRLMUCW-SDNJGBRXSA-
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| InChi Code |
InChI=1S/C48H54N7O8P/c1-33(2)55(34(3)4)64(61-27-13-26-49)63-41-28-44(54-32-52-45-46(50-31-51-47(45)54)53-43(56)30-59-40-16-11-8-12-17-40)62-42(41)29-60-48(35-14-9-7-10-15-35,36-18-22-38(57-5)23-19-36)37-20-24-39(58-6)25-21-37/h7-12,14-25,31-34,41-42,44H,13,27-30H2,1-6H3,(H,50,51,53,56)/t41-,42+,44+,64?/m0/s1
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| Chemical Name |
N-[9-[(2R,4S,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-4-[2-cyanoethoxy-[di(propan-2-yl)amino]phosphanyl]oxyoxolan-2-yl]purin-6-yl]-2-phenoxyacetamide
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| Synonyms |
DMT-dA(PAc) Phosphoramidite
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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 (~112.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.82 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 (2.82 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 | 1.1262 mL | 5.6309 mL | 11.2618 mL | |
| 5 mM | 0.2252 mL | 1.1262 mL | 2.2524 mL | |
| 10 mM | 0.1126 mL | 0.5631 mL | 1.1262 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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