| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
DMT-2'fluoro-da(bz) amidite targets RNA. As a 2'-deoxy-2'-fluorophosphorothioate oligonucleotide, it is designed to bind to complementary RNA sequences with high affinity and specificity. The 2'-fluoro modification enhances nuclease resistance, making it a potent antisense compound. The phosphorothioate backbone further increases stability against enzymatic degradation. Its mechanism involves binding to target RNA and inhibiting its function, such as translation or splicing.
|
|---|---|
| ln Vitro |
The in vitro activity of DMT-2'fluoro-da(bz) amidite is assessed by its utility as a building block for antisense oligonucleotides. The resulting 2'-fluoro-modified oligonucleotides are evaluated for their binding affinity to complementary RNA targets using thermal melting (Tm) analysis. Nuclease resistance is assessed by incubation with various nucleases. The compound's ability to be incorporated into oligonucleotides with high efficiency is also a key measure of its utility.
|
| ln Vivo |
In vivo studies for DMT-2'fluoro-da(bz) amidite are conducted on the antisense oligonucleotides synthesized using this building block rather than the amidite itself. These oligonucleotides are evaluated in animal models for their pharmacokinetic properties, biodistribution, and therapeutic efficacy in applications such as gene silencing or antisense therapy. The 2'-fluoro modification enhances metabolic stability, potentially improving their in vivo performance.
|
| Enzyme Assay |
For oligonucleotide synthesis, DMT-2'fluoro-da(bz) amidite is used in standard solid-phase synthesis protocols. The compound is dissolved in anhydrous acetonitrile and coupled to the growing oligonucleotide chain. Coupling efficiency is monitored by trityl cation release measurements. After synthesis, the oligonucleotide is cleaved from the solid support and deprotected. The final modified oligonucleotide is purified by HPLC or PAGE and characterized by mass spectrometry.
|
| Cell Assay |
For cellular studies, cultured cells are treated with antisense oligonucleotides synthesized using DMT-2'fluoro-da(bz) amidite. Cells are incubated with oligonucleotides for 24-72 hours, and cellular uptake is assessed by fluorescence microscopy or flow cytometry using fluorescently labeled oligonucleotides. Gene knockdown efficiency is evaluated by qRT-PCR or Western blot to assess the antisense activity. Cytotoxicity is assessed using MTT or CellTiter-Glo assays.
|
| Animal Protocol |
For in vivo evaluation of antisense oligonucleotides, 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, with disease biomarkers or survival monitored over time.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of DMT-2'fluoro-da(bz) amidite are characterized for the antisense oligonucleotides incorporating this building block. The compound has a molecular weight of 875.92 and a purity of 98% by HPLC. It is typically handled as a solid and stored at 0-10°C under inert gas to maintain stability. Detailed PK parameters depend on the specific oligonucleotide sequence and backbone chemistry.
|
| Toxicity/Toxicokinetics |
The toxicity profile of DMT-2'fluoro-da(bz) amidite is not explicitly detailed in the provided sources. As a chemical reagent, standard laboratory safety precautions should be followed when handling it. It is intended for research use only and is not for human therapeutic applications. The compound's safety would be evaluated in the context of the final oligonucleotide product rather than the amidite itself.
|
| References | |
| Additional Infomation |
DMT-2'fluoro-da(bz) amidite is a 2'-deoxy-2'-fluorophosphorothioate oligonucleotide building block with a molecular formula of C47H51FN7O7P. It is a potent nuclease-resistant antisense compound that targets RNA with high affinity and specificity. This research compound is for laboratory use only and has not been approved for clinical applications.
|
| Molecular Formula |
C47H51FN7O7P
|
|---|---|
| Molecular Weight |
875.92
|
| Exact Mass |
875.357
|
| CAS # |
136834-22-5
|
| PubChem CID |
12042896
|
| Appearance |
White to off-white solid powder
|
| LogP |
10.49
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
19
|
| Heavy Atom Count |
63
|
| Complexity |
1420
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CC(C)N(C(C)C)P(OCCC#N)O[C@@H]1[C@H](O[C@H]([C@@H]1F)N2C=NC3=C(N=CN=C32)NC(=O)C4=CC=CC=C4)COC(C5=CC=CC=C5)(C6=CC=C(C=C6)OC)C7=CC=C(C=C7)OC
|
| InChi Key |
VCCMVPDSLHFCBB-MSIRFHFKSA-N
|
| InChi Code |
InChI=1S/C47H51FN7O7P/c1-31(2)55(32(3)4)63(60-27-13-26-49)62-42-39(61-46(40(42)48)54-30-52-41-43(50-29-51-44(41)54)53-45(56)33-14-9-7-10-15-33)28-59-47(34-16-11-8-12-17-34,35-18-22-37(57-5)23-19-35)36-20-24-38(58-6)25-21-36/h7-12,14-25,29-32,39-40,42,46H,13,27-28H2,1-6H3,(H,50,51,53,56)/t39-,40-,42-,46-,63?/m1/s1
|
| Chemical Name |
N-[9-[(2R,3R,4R,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-4-[2-cyanoethoxy-[di(propan-2-yl)amino]phosphanyl]oxy-3-fluorooxolan-2-yl]purin-6-yl]benzamide
|
| Synonyms |
DMT-2'fluoro-da(bz) amidite
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~114.2 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.85 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 | 1.1417 mL | 5.7083 mL | 11.4166 mL | |
| 5 mM | 0.2283 mL | 1.1417 mL | 2.2833 mL | |
| 10 mM | 0.1142 mL | 0.5708 mL | 1.1417 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
