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Letermovir (AIC246) CMV inhibitor

Name: Letermovir (AIC246)
Brand: Selleck Chemicals
SKU: S8873
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S8873

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.

Chemical Structure

Molecular Weight: 572.55

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.87

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV Neuraminidase HCV HSV RSV Enterovirus Thioredoxin Reductase 3C-Like Protease Ribosomal Peptidyl Transferase HPV
Related Products	Valaciclovir HCl Bisindolylmaleimide IV

Chemical Information, Storage & Stability

Molecular Weight	572.55	Formula	C₂₉H₂₈F₄N₄O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	917389-32-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-8228			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

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (8.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (1.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

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	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].
References	https://pubmed.ncbi.nlm.nih.gov/21752907/ https://pubmed.ncbi.nlm.nih.gov/20047911/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

Tech Support

Handling Instructions

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