1. Anti-infection
  2. RSV

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

Cat. No.: HY-12983A Purity: >98.0%
Handling Instructions

ALS-8176 an inhibitor of the respiratory syncytial virus (RSV) polymerase.

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

ALS-8176 Chemical Structure

ALS-8176 Chemical Structure

CAS No. : 1445385-02-3

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

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ALS-8176 an inhibitor of the respiratory syncytial virus (RSV) polymerase.

In Vitro

ALS-008176 is an orally bioavailable prodrug of the novel RSV replication inhibitor ALS-008112, a cytidine nucleoside analogue[1].

In Vivo

ALS-8176 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. ALS-8176 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 ALS-8176 to monkeys[2]. In an adult human challenge study, ALS-8176 has shown efficacy against RSV infection[1].

Clinical Trial
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    90% corn oil

    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    40% PEG300    5% Tween-80    45% saline

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

References
Kinase Assay
[2]

Cell fractionation and extraction of RSV RNP complex is performed. Nucleoside triphosphate (NTP) concentrations are: 0.1 μM CTP and 1 μM ATP, 2 μM UTP, and 500 μM GTP. The radioactive tracer is either 10 μCi [α-33P]rCTP or 15 μCi

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

Animal Administration
[2]

Rats: ALS-8176 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: ALS-8176 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
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
ALS-8176
Cat. No.:
HY-12983A
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ALS-8176

Cat. No.: HY-12983A