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

Name: Lumicitabine
Brand: MedChemExpress
SKU: HY-12983A
Rating: 5.0 (1 reviews)

Cat. No.: HY-12983A Purity: 99.34%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1445385-02-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 401	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 401	In-stock	Estimated Time of Arrival: December 31
Solid
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
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lumicitabine:

ALS-8112 In-stock

1 Publications Citing Use of MCE Lumicitabine

•Microorganisms. 2023 Jun 18, 11(6), 1608.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	CC₅₀	> 100 μM Compound: 71, ALS-8176	Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay	[PMID: 25667954]
HeLa	EC₅₀	0.26 μM Compound: 71, ALS-8176	Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay	[PMID: 25667954]

In Vitro

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

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

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].

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

Clinical Trial

Molecular Weight

433.86

Formula

C₁₈H₂₅ClFN₃O₆

CAS No.

1445385-02-3

Appearance

Solid

Color

White to off-white

SMILES

ClC[C@@]1(COC(C(C)C)=O)[C@@H](OC(C(C)C)=O)[C@@H](F)[C@H](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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (115.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.34%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (258 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. [Content Brief]

[2]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. [Content Brief]

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

[1]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. [Content Brief]

[2]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3049 mL	11.5245 mL	23.0489 mL	57.6223 mL
	5 mM	0.4610 mL	2.3049 mL	4.6098 mL	11.5245 mL
	10 mM	0.2305 mL	1.1524 mL	2.3049 mL	5.7622 mL
	15 mM	0.1537 mL	0.7683 mL	1.5366 mL	3.8415 mL
	20 mM	0.1152 mL	0.5762 mL	1.1524 mL	2.8811 mL
	25 mM	0.0922 mL	0.4610 mL	0.9220 mL	2.3049 mL
	30 mM	0.0768 mL	0.3841 mL	0.7683 mL	1.9207 mL
	40 mM	0.0576 mL	0.2881 mL	0.5762 mL	1.4406 mL
	50 mM	0.0461 mL	0.2305 mL	0.4610 mL	1.1524 mL
	60 mM	0.0384 mL	0.1921 mL	0.3841 mL	0.9604 mL
	80 mM	0.0288 mL	0.1441 mL	0.2881 mL	0.7203 mL
	100 mM	0.0230 mL	0.1152 mL	0.2305 mL	0.5762 mL

Lumicitabine Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lumicitabine1445385-02-3ALS-008176 ALS-8176ALS008176ALS 008176ALS8176ALS 8176ALS-8176RSVRespiratory syncytial virusInhibitorinhibitorinhibit

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

Customer Review

Other Forms of Lumicitabine:

Lumicitabine Related Antibodies

1 Publications Citing Use of MCE Lumicitabine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Lumicitabine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Lumicitabine Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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