Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
Other Sizes |
|
ln Vitro |
HCV replicon cells are treated with 10 μM 3H-labeled NHC in an intracellular metabolism test. After 1, 2, and 8 hours of incubation, intracellular nucleotide levels are measured. NHC is quickly transformed into the mono-, di-, and triphosphate forms; within 8 hours, NHC-TP can reach 71.12 pM[1]. In the absence of NHC-triphosphate tetraammonium (NHC-TP) (3-5 μM), full-length polymerization products result, and it may be a poor substitute substrate. Furthermore, in cell-free HCV NS5B polymerization events, an evident electrophoretic shift is seen, and the molecular weight of the polymerization product increases by 16 (one extra oxygen) upon insertion of NHC-TP rather than CTP[1]. NHC (10–50 μM; 4 h) or a McGuigan phosphoramidate prodrug of NHC are cultured in Huh-7 cells. LC-MS/MS is used to evaluate the intracellular levels of the primary chemicals and phosphorylated metabolites. While NHC-triphosphate tetraammonium continues to be the most prevalent metabolite, trace levels of NHC-monophosphate (MP) and NHC-diphosphate (DP) are also visible[2]. The metabolite NHC-triphosphate tetraammonium (NHC-TP) may act as a nonobligate chain terminator and directly target the viral polymerase. Through chain termination or mutagenesis, it inhibits early negative-strand RNA synthesis in a significant way. This can potentially obstruct the proper assembly of replicase complexes.
|
---|---|
References |
Molecular Formula |
C9H28N7O15P3
|
---|---|
Molecular Weight |
567.28
|
Related CAS # |
NHC-triphosphate;34973-27-8;NHC-triphosphate tetrasodium
|
Appearance |
White to off-white solid powder
|
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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). 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)
|
Solubility (In Vitro) |
H2O :~200 mg/mL (~352.56 mM)
DMSO :~170 mg/mL (~299.68 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.25 mg/mL (7.49 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 42.5 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: ≥ 4.25 mg/mL (7.49 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 42.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 100 mg/mL (176.28 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7628 mL | 8.8140 mL | 17.6280 mL | |
5 mM | 0.3526 mL | 1.7628 mL | 3.5256 mL | |
10 mM | 0.1763 mL | 0.8814 mL | 1.7628 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.