ALS-8112

Name: ALS-8112
Brand: MedChemExpress
SKU: HY-12983
Rating: 5.0 (3 reviews)

Cat. No.: HY-12983 Purity: 98.90%: FAQs
Data Sheet SDS COA Handling Instructions

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ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC₅₀ of 0.02 μM.

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

ALS-8112 Chemical Structure

CAS No. : 1445379-92-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 581	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 581	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 3 publication(s) in Google Scholar

Other Forms of ALS-8112:

Lumicitabine In-stock

2 Publications Citing Use of MCE ALS-8112

Proliferation Assay

: ALS-8112 purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2018 Feb;150:79-92. [Abstract]; To confirm the antiviral effect of StA-NS2-2, infectious titer produced from compound-treated A549 cells and IFN-deficient Vero cells are examined. The RSV polymerase inhibitor ALS-8112 potently inhibits RSV in both cell types.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC₅₀ of 0.02 μM.

IC₅₀ & Target

IC50: 0.02 μM (RSV)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	CC₅₀	> 100 μM Compound: 2c	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	0.15 μM Compound: 2c	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]
HEp-2	CC₅₀	> 100 μM Compound: ALS-8112	Cytotoxicity against human Hep2 cells assessed as reduction in cell viability measured after 5 days by MTS assay Cytotoxicity against human Hep2 cells assessed as reduction in cell viability measured after 5 days by MTS assay	[PMID: 32143992]
HEp-2	EC₅₀	0.92 μM Compound: 15	Antiviral activity against RSV A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay Antiviral activity against RSV A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay	[PMID: 25978965]
HEp-2	IC₅₀	1 μM Compound: 15	Inhibition of RSV A2 RNA-dependent RNA polymerase expressed in human Hep2 cells using ATP, GTP, UTP, CTP and 1.5 uCi [alpha-32P] NTP as substrate assessed as reduction of total radiolabled transcript after 90 mins by agarose gel electrophoresis Inhibition of RSV A2 RNA-dependent RNA polymerase expressed in human Hep2 cells using ATP, GTP, UTP, CTP and 1.5 uCi [alpha-32P] NTP as substrate assessed as reduction of total radiolabled transcript after 90 mins by agarose gel electrophoresis	[PMID: 25978965]
HEp-2	EC₅₀	2.6 μM Compound: ALS-8112	Antiviral activity against Respiratory syncytial virus A strain Long infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis Antiviral activity against Respiratory syncytial virus A strain Long infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis	[PMID: 32143992]
HEp-2	EC₅₀	2.6 μM Compound: ALS-8112	Antiviral activity against Respiratory syncytial virus B infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis Antiviral activity against Respiratory syncytial virus B infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis	[PMID: 32143992]
MT4	CC₅₀	21 μM Compound: 15	Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by Cell-Titer Glo assay Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by Cell-Titer Glo assay	[PMID: 25978965]

In Vitro

The 5'-triphosphate form of ALS-8112 (ALS-8112-TP) is the active form of the drug and selectively inhibits RSV polymerase through chain termination of RNA synthesis^[2]. ALS-008112 enters various types of epithelial cells in the respiratory tract and is subsequently phosphorylated to form an intracellular nucleoside triphosphate with a half-life of approximately 29 hours. The nucleoside triphosphate analogue inhibits RSV replication by means of chain termination^[3]. ALS-8112 is a pan-strain inhibitor of RSV replication in vitro. The RNA transcription activity of the RSV–RNP complex is dose-proportionally inhibited by ALS-8112-TP with an IC₅₀ of 0.020 ± 0.008 μM^[4].

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

Molecular Weight

293.68

Formula

C₁₀H₁₃ClFN₃O₄

CAS No.

1445379-92-9

Appearance

Solid

Color

White to off-white

SMILES

OC[C@]1(CCl)[C@@H](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 : ≥ 47 mg/mL (160.04 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	3.4051 mL	17.0253 mL	34.0507 mL
5 mM	0.6810 mL	3.4051 mL	6.8101 mL
10 mM	0.3405 mL	1.7025 mL	3.4051 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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution

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: 98.90%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (257 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. 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]

[2]. Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91. [Content Brief]

[3]. 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]

[4]. Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995. [Content Brief]

Cell Assay
^[4]

ALS-8112 and its prodrug ALS-8176 are stored at 4°C in dimethyl sulfoxide (DMSO), and diluted in water. HEp-2 cells per well are plated in a 96-well plate. Each compound is serially diluted (1:3) up to 9 distinct concentrations. Cells are pre-incubated with compounds for 24 hours at 37°C in a 5% CO₂ atmosphere. After 24 hours of pre-incubation with compounds, RSV A2, Long, or B1 at a multiplicity of infection (MOI) of 0.5 is added to the cells, except for the background controls. The plate is then incubated for additional 4 days in the same conditions and at the end of the incubation 50 μL the supernatant from each well of the plate is collected^[4].

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

References

[1]. 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]

[2]. Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91. [Content Brief]

[3]. 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]

[4]. Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.4051 mL	17.0253 mL	34.0507 mL	85.1267 mL
	5 mM	0.6810 mL	3.4051 mL	6.8101 mL	17.0253 mL
	10 mM	0.3405 mL	1.7025 mL	3.4051 mL	8.5127 mL
	15 mM	0.2270 mL	1.1350 mL	2.2700 mL	5.6751 mL
	20 mM	0.1703 mL	0.8513 mL	1.7025 mL	4.2563 mL
	25 mM	0.1362 mL	0.6810 mL	1.3620 mL	3.4051 mL
	30 mM	0.1135 mL	0.5675 mL	1.1350 mL	2.8376 mL
	40 mM	0.0851 mL	0.4256 mL	0.8513 mL	2.1282 mL
	50 mM	0.0681 mL	0.3405 mL	0.6810 mL	1.7025 mL
	60 mM	0.0568 mL	0.2838 mL	0.5675 mL	1.4188 mL
	80 mM	0.0426 mL	0.2128 mL	0.4256 mL	1.0641 mL
	100 mM	0.0341 mL	0.1703 mL	0.3405 mL	0.8513 mL

ALS-8112 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:

ALS-81121445379-92-9ALS8112ALS 8112RSVRespiratory syncytial virusInhibitorinhibitorinhibit

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ALS-8112

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Other Forms of ALS-8112:

ALS-8112 Related Antibodies

2 Publications Citing Use of MCE ALS-8112

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Protocol

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References

Customer Review

ALS-8112 Related Antibodies

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Complete Stock Solution Preparation Table

ALS-8112 Related Classifications

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