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Letermovir (AIC246)

Name: Letermovir (AIC246)
Brand: Selleck Chemicals
SKU: S8873
Rating: 5 (2 reviews)

Synonyms: MK-8228

Catalog No.S8873 Purity:99.87%

Letermovir (AIC246, MK-8228) is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

Letermovir (AIC246) Chemical Structure

CAS No. 917389-32-3

Purity & Quality Control

Batch: S887301 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.87%

99.87

Letermovir (AIC246) Related Products

Related Targets	HCMV	Click to Expand
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Related Compound Libraries	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	Click to Expand

Biological Activity

Description	Letermovir (AIC246, MK-8228) is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

In vitro
In vitro	AIC246 blocks viral replication without inhibiting the synthesis of progeny HCMV DNA or viral proteins. It is one of the most potent anti-HCMV agents reported to date, with a cell culture EC50 in the one-digit nanomolar range (∼5 nM) and a selectivity index exceeding 15,000^[1].

In Vivo
In vivo	AIC246 treatment leads to a dose-dependent reduction of the HCMV titer in transplanted cells compared to that of the placebo-treated control group using the mouse xenograft model^[2].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06118515	Not yet recruiting	Congenital Cytomegalovirus Infection	National Institute of Allergy and Infectious Diseases (NIAID)	November 16 2023	Phase 1
NCT06057194	Not yet recruiting	Infections Cytomegalovirus	Maimónides Biomedical Research Institute of Córdoba\|MERCK SHARP & DOHME DE ESPAÑA S.A.	October 2023	Phase 2
NCT05446571	Recruiting	Pregnant Women\|CMV Infected Fetuses	Assistance Publique - Hôpitaux de Paris	October 20 2023	Phase 3
NCT06001320	Recruiting	Kidney Transplant; Complications\|CMV	Virginia Commonwealth University\|Merck Sharp & Dohme LLC	September 25 2023	Early Phase 1
NCT05626530	Recruiting	Cytomegalovirus Infections\|Infection in Solid Organ Transplant Recipients\|Neutropenia\|Antiviral Toxicity	Tufts Medical Center	February 2 2023	Phase 4

References

Chemical Information & Solubility

Molecular Weight	572.55	Formula	C₂₉H₂₈F₄N₄O₄
CAS No.	917389-32-3	SDF	--
Smiles	COC1=C(C=C(C=C1)C(F)(F)F)N2C(C3=C(C(=CC=C3)F)N=C2N4CCN(CC4)C5=CC(=CC=C5)OC)CC(=O)O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (174.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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