1. Anti-infection
  2. CMV
  3. Letermovir

Letermovir (Synonyms: AIC246)

Cat. No.: HY-15233 Purity: 98.75% ee.: 99.91
Handling Instructions

Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

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

Letermovir Chemical Structure

Letermovir Chemical Structure

CAS No. : 917389-32-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 378 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Top Publications Citing Use of Products

    Letermovir purchased from MCE. Usage Cited in: Eur J Pharm Sci. 2019 Jan 15;127:29-37.

    Viral reporter GFP expression after inoculation and compound treatment. Infected cells treated with DMSO control, BIO, Ganciclovir (GCV) or Letermovir (LTR)
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

    In Vitro

    AIC246 has consistent antiviral efficacy, and there is remarkable selectivity of AIC246 for human cytomegaloviruses[1]. AD169 mutant strains and designated rAIC246-1 and rAIC246-2 are highly resistant to Letermovir (AIC246), with EC50s of 5.6 nM, 1.24 μM, 0.37 μM, respectively. Letermovir inhibits HCMV replication through a specific antiviral mechanism that involves the viral gene product UL56. Letermovir inhibits HCMV replication in cell culture by interfering with the proper cleavage/packaging of HCMV progeny DNA[2]. Letermovir inhibits the current gold standard GCV by more than 400-fold with respect to EC50s (mean, 4.5 nM versus 2 μM) and by more than 2,000-fold with respect to EC90 values (mean, 6.1 nM versus 14.5 μM)[3]. Letermovir in conbination with anti-HCMV drugs causes additive antiviral effects, but there is no interaction between letermovir and anti-HIV drugs[4].

    In Vivo

    Letermovir (10-100 mg/kg/day, p.o.) 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[3].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (174.66 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7466 mL 8.7329 mL 17.4657 mL
    5 mM 0.3493 mL 1.7466 mL 3.4931 mL
    10 mM 0.1747 mL 0.8733 mL 1.7466 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    Briefly, 5×103 AD169-infected NHDF cells/well are seeded into the wells of 30 96-well microtiter plates. The infection is allowed to proceed under the exposure of 50 nM AIC246 (10×EC50) until a CPE developed in one or more of the compound-treated wells (indicative of resistant virus breakthrough). Noninfected and nontreated cells serve as controls on each plate. Mutant virus amplification is accomplwashed after cultures achieved maximum CPE by the passage of cell-free supernatant virus in the presence of 50 nM AIC246. The resultant AIC246-resistant progeny virus mutants are plaque purified three times by limiting dilutions in the presence of AIC246. The stability of resistance is tested by serially passaging plaque-purified viruses without selective pressure (8 to 10 times). 

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

    Animal Administration
    [3]

    Mice (18 to 25 g body weight) are anesthetized, and the Gelfoam sponges are implanted subcutaneously in the dorsoscapular area. After transplantation, mice are randomized and grouped in 10 animals per treatment group. Starting 4 h after transplantation, mice are treated once daily with letermovir for nine consecutive days. Drugs are applied per os by oral gavage. Total administration volume is 10 mL/kg. Mice are sacrificed after 9 days of treatment, and the Gelfoam implants are removed and digested with collagenase at 37°C. After 2 to 3 h, human cells are recovered by centrifugation and resuspended in GM. Subsequently, the isolated cell suspensions are serially diluted and mixed with uninfected NHDF indicator cells and PFU are determined by plaque assays as described above. Virus titers determined from isolated cells are given as PFU/mL.

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

    References
    Molecular Weight

    572.55

    Formula

    C₂₉H₂₈F₄N₄O₄

    CAS No.

    917389-32-3

    SMILES

    FC1=C(N=C(N2CCN(C3=CC=CC(OC)=C3)CC2)N(C4=CC(C(F)(F)F)=CC=C4OC)[[email protected]]5CC(O)=O)C5=CC=C1

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Letermovir
    Cat. No.:
    HY-15233
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    Letermovir

    Cat. No.: HY-15233