| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Lumicitabine targets the respiratory syncytial virus (RSV) RNA polymerase. It acts as a chain terminator, inhibiting viral RNA synthesis. The compound is a cytidine nucleoside analog that is phosphorylated to the active triphosphate form.
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| ln Vitro |
Lumicitabine is a cytidine nucleoside analog and an orally accessible prodrug of ALS-008112, a new RSV replication inhibitor [1].
In vitro, lumicitabine inhibits RSV replication in cell culture. The compound shows potent antiviral activity against RSV with low cytotoxicity. It is active against a range of RSV strains. |
| ln Vivo |
Excellent anti-RSV efficacy and safety were shown by lumicitabine in a Phase 2 clinical RSV challenge investigation. It has a high body level of 2c-TP and strong oral absorption. In addition to simulating stomach and intestinal fluids (half-life >2 hours), lumicitabine has exceptional formulation stability (storage stability in 0.5% methylcellulose aqueous formulation at room temperature >24 hours). It can be taken orally in solutions and aqueous suspensions containing comparatively small amounts of organic solvents due to its considerable solubility. Oral Lumicitabine treatment results in high amounts of NMP and NTP in monkeys[2]. In an adult challenge investigation, lumicitabine showed effectiveness against RSV infection [1].
In vivo, lumicitabine has been studied in animal models of RSV infection. It shows efficacy in reducing viral load and improving clinical outcomes. The compound has been evaluated in clinical trials for the treatment of RSV infection. |
| Enzyme Assay |
In vitro enzyme assays measure the inhibition of RSV RNA polymerase activity. Lumicitabine triphosphate is incubated with RSV polymerase and a RNA template, and incorporation of the nucleotide analog is measured. The IC50 for polymerase inhibition is determined.
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| Cell Assay |
In vitro cellular assays evaluate the antiviral activity of lumicitabine against RSV in cell culture. Cells are infected with RSV and treated with varying concentrations of the compound. Viral replication is measured by plaque assay, qPCR, or immunofluorescence to determine the EC50.
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| Animal Protocol |
In vivo animal experiments are conducted in mouse or cotton rat models of RSV infection. Lumicitabine is administered orally or by other routes, and viral load in lung tissue is measured. Efficacy is assessed by reduction in viral titer and improvement in clinical signs.
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| ADME/Pharmacokinetics |
Lumicitabine has a molecular formula of C20H25FN4O7 and a molecular weight of 452.43. It has a CAS number of 1445385-02-3. The compound is a cytidine nucleoside analog prodrug that is orally bioavailable.
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| Toxicity/Toxicokinetics |
The toxicity profile of lumicitabine is consistent with that of other nucleoside analogs. Potential side effects may include gastrointestinal effects and myelosuppression. The compound has been evaluated in clinical trials for safety and efficacy.
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| References |
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| Additional Infomation |
Lumicitabine is currently being investigated in clinical trial NCT03010059 (a study evaluating the relative bioavailability of two different novel concept formulations (oral suspension and tablets) compared to their respective existing formulations, as well as assessing the effect of food on the pharmacokinetics of these two novel concept formulations).
Drug Indication Treatment of lower respiratory tract diseases caused by human respiratory syncytial virus (RSV) Lumicitabine was being developed for the treatment of respiratory syncytial virus (RSV) infection. It is a cytidine nucleoside analog that inhibits RSV replication. Clinical trials have been conducted to evaluate its safety and efficacy in patients with RSV infection. |
| Molecular Formula |
C18H25CLFN3O6
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|---|---|
| Molecular Weight |
433.86
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| Exact Mass |
433.141
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| CAS # |
1445385-02-3
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| Related CAS # |
ALS-8112;1445379-92-9
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| PubChem CID |
89658382
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
533.5±60.0 °C at 760 mmHg
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| Flash Point |
276.4±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
2.31
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
29
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| Complexity |
728
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)C(=O)OC[C@@]1([C@H]([C@H]([C@@H](O1)N2C=CC(=NC2=O)N)F)OC(=O)C(C)C)CCl
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| InChi Key |
MJVKYGMNSQJLIN-KYZVSKTDSA-N
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| InChi Code |
InChI=1S/C18H25ClFN3O6/c1-9(2)15(24)27-8-18(7-19)13(28-16(25)10(3)4)12(20)14(29-18)23-6-5-11(21)22-17(23)26/h5-6,9-10,12-14H,7-8H2,1-4H3,(H2,21,22,26)/t12-,13+,14-,18-/m1/s1
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| Chemical Name |
[(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-2-(chloromethyl)-4-fluoro-3-(2-methylpropanoyloxy)oxolan-2-yl]methyl 2-methylpropanoate
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| Synonyms |
ALS8176； ALS 8176; ALS-8176; Lumicitabine
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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 |
| 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 (~115.24 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.76 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 (5.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3049 mL | 11.5245 mL | 23.0489 mL | |
| 5 mM | 0.4610 mL | 2.3049 mL | 4.6098 mL | |
| 10 mM | 0.2305 mL | 1.1524 mL | 2.3049 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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