1. Anti-infection
  2. RSV
  3. Lumicitabine

Lumicitabine (Synonyms: ALS-008176; ALS-8176)

Cat. No.: HY-12983A Purity: 99.78%
Handling Instructions

Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.

For research use only. We do not sell to patients.

Lumicitabine Chemical Structure

Lumicitabine Chemical Structure

CAS No. : 1445385-02-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 401 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.

In Vitro

Lumicitabine is an orally bioavailable prodrug of the novel RSV replication inhibitor ALS-008112, a cytidine nucleoside analogue[1].

In Vivo

Lumicitabine demonstrates excellent anti-RSV efficacy and safety in a phase 2 clinical RSV challenge study. It exhibits good oral bioavailability and a high level of 2c-TP in vivo. Lumicitabine has excellent stability profiles in formulations (>24 h storage stability in 0.5% methylcellulose aqueous formulation at rt) and simulats gastric and intestinal fluids (half-life >2 h). Its solubility is adequate to support oral administration in solutions with relatively low percentage of organic solvent and in aqueous suspensions. High levels of NMP and NTP are obtained following oral administration of Lumicitabine to monkeys[2]. In an adult human challenge study, Lumicitabine has shown efficacy against RSV infection[1].

Clinical Trial
Molecular Weight

433.86

Formula

C₁₈H₂₅ClFN₃O₆

CAS No.

1445385-02-3

SMILES

ClC[[email protected]@]1(COC(C(C)C)=O)[[email protected]@H](OC(C(C)C)=O)[[email protected]@H](F)[[email protected]](N2C(N=C(N)C=C2)=O)O1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (115.24 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Rats: Lumicitabine are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies are conducted at 5 mg/kg and for oral PK studies the prodrugs are administered at 5 mg/kg parent nucleoside equivalent doses. Blood samples are typically collected at various time points up to 24 h post dose for rat[2].

Monkeys: Lumicitabine are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies are conducted at 5 mg/kg and for oral PK studies the prodrugs are administered at 5 mg/kg parent nucleoside equivalent doses. Blood samples are typically collected at various time points up to 12 h post dose for Monkeys[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.78%

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Lumicitabine
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HY-12983A
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