| Size | Price | Stock | Qty |
|---|---|---|---|
| 1g |
|
||
| Other Sizes |
| Targets |
Not applicable; this is a chemical building block for oligonucleotide synthesis. The resulting MOE-modified antisense oligonucleotides (ASOs) target complementary RNA sequences via Watson-Crick base pairing, with increased nuclease resistance and RNA affinity.
|
|---|---|
| ln Vitro |
Not applicable; as a monomer, it has no direct biological activity. Incorporation of 2'-MOE modifications into ASOs increases melting temperature (Tm) by 2-5degC per modification, enhances nuclease resistance (10-1000-fold), and reduces immunostimulatory potential.
|
| ln Vivo |
Not applicable; the amidite monomer is not administered. MOE-modified ASOs (e.g., nusinersen) show improved in vivo stability (terminal half-life of 2-4 weeks in tissues) and efficacy in animal models of genetic diseases.
|
| Enzyme Assay |
The phosphoramidite (0.1 M in acetonitrile) is coupled to a solid support-bound oligonucleotide using standard phosphoramidite chemistry. Activator (e.g., 5-ethylthio-1H-tetrazole, 0.25 M) is added for 5-15 minutes, followed by oxidation (0.02 M I2 in THF/water/pyridine), capping, and detritylation (3% TCA in DCM).
|
| Cell Assay |
Not applicable; the amidite monomer is not tested in cells. The fully synthesized MOE-modified ASO (10-200 nM) is transfected into cells using cationic lipids (e.g., Lipofectamine 2000). Target mRNA knockdown is measured by qRT-PCR after 24-72 hours; protein reduction is assessed by Western blot or ELISA.
|
| Animal Protocol |
Not applicable for amidite. MOE-ASOs are administered to mice via subcutaneous or intravenous injection (10-100 mg/kg, 1-3 times weekly) for 1-8 weeks. Tissues (liver, kidney, muscle, brain) are collected for PK (LC-MS/MS) and pharmacodynamic (target mRNA by qPCR) analyses.
|
| ADME/Pharmacokinetics |
Not applicable for amidite. MOE-ASOs exhibit high plasma protein binding (90-99%), a distribution half-life of 0.5-2 hours, and a terminal elimination half-life of 1-4 weeks in tissues (liver, kidney). Renal excretion of full-length ASO is minimal (<5% of dose).
|
| Toxicity/Toxicokinetics |
No toxicity data for amidite. For MOE-ASOs, high doses (>100 mg/kg weekly) in rodents may cause hepatotoxicity (elevated ALT/AST), nephrotoxicity (proximal tubule degeneration), and thrombocytopenia. The amidite should be handled as a chemical irritant.
|
| References | |
| Additional Infomation |
DMT-2'O-MOE-rG(ib) amidite is a research-use reagent not intended for clinical use. 2'-MOE modification is a clinically validated chemistry used in FDA-approved ASOs (e.g., nusinersen for spinal muscular atrophy, inotersen for hereditary transthyretin amyloidosis). This building block enables synthesis of therapeutic oligonucleotides.
|
| Molecular Formula |
C47H60N7O10P
|
|---|---|
| Molecular Weight |
913.99397277832
|
| Exact Mass |
913.414
|
| CAS # |
251647-55-9
|
| PubChem CID |
136745830
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.403
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
23
|
| Heavy Atom Count |
65
|
| Complexity |
1550
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CC(C)C(=O)NC1=NC2=C(C(=O)N1)N=CN2[C@H]3[C@@H]([C@@H]([C@H](O3)COC(C4=CC=CC=C4)(C5=CC=C(C=C5)OC)C6=CC=C(C=C6)OC)OP(N(C(C)C)C(C)C)OCCC#N)OCCOC
|
| InChi Key |
LADCDGNEBIQAAU-SBCRAQIVSA-N
|
| InChi Code |
InChI=1S/C47H60N7O10P/c1-30(2)43(55)51-46-50-42-39(44(56)52-46)49-29-53(42)45-41(60-27-26-57-7)40(64-65(62-25-13-24-48)54(31(3)4)32(5)6)38(63-45)28-61-47(33-14-11-10-12-15-33,34-16-20-36(58-8)21-17-34)35-18-22-37(59-9)23-19-35/h10-12,14-23,29-32,38,40-41,45H,13,25-28H2,1-9H3,(H2,50,51,52,55,56)/t38-,40-,41-,45-,65?/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-(2-methoxyethoxy)oxolan-2-yl]-6-oxo-1H-purin-2-yl]-2-methylpropanamide
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~273.53 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0941 mL | 5.4705 mL | 10.9410 mL | |
| 5 mM | 0.2188 mL | 1.0941 mL | 2.1882 mL | |
| 10 mM | 0.1094 mL | 0.5471 mL | 1.0941 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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