Letermovir
Based on 20 publication(s) in Google Scholar
Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
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- Purity: 99.96%
- CAS No.: 917389-32-3
- 화학식: C29H28F4N4O4
- 분자량:572.55
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Letermovir
More- PLoS Pathog. 2017 Feb 27;13(2):e1006202. [Abstract]
- Eur J Pharm Sci. 2019 Jan 15:127:29-37. [Abstract]
- Antimicrob Agents Chemother. 2020 Dec 16;65(1):e01627-20. [Abstract]
- Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00922-18. [Abstract]
- Antimicrob Agents Chemother. 2015 Oct;59(10):6588-93. [Abstract]
- Antiviral Res. 2025 Dec:244:106289. [Abstract]
- Antiviral Res. 2022 Aug:204:105361. [Abstract]
- Antiviral Res. 2019 Dec;172:104639. [Abstract]
- Antiviral Res. 2018 Oct:158:255-263. [Abstract]
- Antiviral Res. 2018 Sep:157:128-133. [Abstract]
- Antiviral Res. 2017 Dec:148:1-4. [Abstract]
- J Virol. 2025 Sep 16:e0117325. [Abstract]
- J Virol. 2017 Jan 18;91(3). pii: e02152-16. [Abstract]
- Bioorg Med Chem. 2023 May 1:85:117276. [Abstract]
- PLoS One. 2020 Apr 30;15(4):e0232140. [Abstract]
- Microbiol Immunol. 2018 Oct;62(10):651-658. [Abstract]
- bioRxiv. 2026 May 4.
- SSRN. 2023 Feb 27.
- Patent. US20210228711A1.
- Johannes Gutenberg University Mainz. 2021 Aug 17.
Customer Validation & Images
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IF
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEL | EC50 |
0.0046 μM
Compound: Letermovir
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Antiviral activity against Cytomegalovirus AD-169 infected in HEL cells assessed as reduction of virus-induced cytopathogenicity
Antiviral activity against Cytomegalovirus AD-169 infected in HEL cells assessed as reduction of virus-induced cytopathogenicity
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[PMID: 26001344] |
| HEL 299 | CC50 |
63 μM
Compound: AIC246
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Cytotoxicity against HEL299 cells infected with human cytomegalovirus after 7 days by alamar blue assay
Cytotoxicity against HEL299 cells infected with human cytomegalovirus after 7 days by alamar blue assay
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[PMID: 20047911] |
| HEL 299 | EC50 |
0.0035 μM
Compound: AIC246
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Antiviral activity against human cytomegalovirus infected in HEL299 cells after 7 days by GFP-based fluorescent reduction assay
Antiviral activity against human cytomegalovirus infected in HEL299 cells after 7 days by GFP-based fluorescent reduction assay
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[PMID: 20047911] |
| HS27 | CC50 |
107 μM
Compound: AIC246
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Cytotoxicity against human HS27 cells infected with human cytomegalovirus after 7 days by alamar blue assay
Cytotoxicity against human HS27 cells infected with human cytomegalovirus after 7 days by alamar blue assay
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[PMID: 20047911] |
| HS27 | EC50 |
0.0056 μM
Compound: AIC246
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Antiviral activity against human cytomegalovirus infected in human HS27 cells after 7 days by GFP-based fluorescent reduction assay
Antiviral activity against human cytomegalovirus infected in human HS27 cells after 7 days by GFP-based fluorescent reduction assay
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[PMID: 20047911] |
| MRC5 | CC50 |
127 μM
Compound: AIC246
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Cytotoxicity against human MRC5 cells infected with human cytomegalovirus after 7 days by alamar blue assay
Cytotoxicity against human MRC5 cells infected with human cytomegalovirus after 7 days by alamar blue assay
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[PMID: 20047911] |
| MRC5 | EC50 |
0.0045 μM
Compound: AIC246
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Antiviral activity against human cytomegalovirus infected in human MRC5 cells after 7 days by GFP-based fluorescent reduction assay
Antiviral activity against human cytomegalovirus infected in human MRC5 cells after 7 days by GFP-based fluorescent reduction assay
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[PMID: 20047911] |
| NHDF | CC50 |
91 μM
Compound: AIC246
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Cytotoxicity against NHDF infected with human cytomegalovirus after 7 days by alamar blue assay
Cytotoxicity against NHDF infected with human cytomegalovirus after 7 days by alamar blue assay
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[PMID: 20047911] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 917389-32-3
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Appearance Solid
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분자량 572.55
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화학식 C29H28F4N4O4
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Color Off-white to yellow
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SMILES
FC1=C(N=C(N2CCN(C3=CC=CC(OC)=C3)CC2)N(C4=CC(C(F)(F)F)=CC=C4OC)[C@H]5CC(O)=O)C5=CC=C1
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Synonyms
AIC246; MK-8228
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (20)
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Journal Impact Factor
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Most Recent
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PLoS Pathog
Replication of CMV in the gut of HIV-infected individuals and epithelial barrier dysfunction. [Abstract]2017 Feb 27;13(2):e1006202. PMID: 28241080 -
Eur J Pharm Sci
FRET-based assay using a three-way junction DNA substrate to identify inhibitors of human cytomegalovirus pUL89 endonuclease activity. [Abstract]2019 Jan 15:127:29-37. PMID: 30342172
Letermovir purchased from MedChemExpress. Usage Cited in: Eur J Pharm Sci. 2019 Jan 15:127:29-37. [Abstract]
Viral reporter GFP expression after inoculation and compound treatment. Infected cells treated with DMSO control, BIO, Ganciclovir (GCV) or Letermovir (LTR)
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Antimicrob Agents Chemother
Investigational Antiviral Therapy Models for the Prevention and Treatment of Congenital Cytomegalovirus Infection during Pregnancy. [Abstract]2020 Dec 16;65(1):e01627-20. PMID: 33077661 -
Antimicrob Agents Chemother
New Locus of Drug Resistance in the Human Cytomegalovirus UL56 Gene Revealed by In Vitro Exposure to Letermovir and Ganciclovir. [Abstract]2018 Aug 27;62(9). pii: e00922-18. PMID: 29914965 -
Antimicrob Agents Chemother
Rapid In Vitro Evolution of Human Cytomegalovirus UL56 Mutations That Confer Letermovir Resistance. [Abstract]2015 Oct;59(10):6588-93. PMID: 26259791 -
Antiviral Res
2025 Dec:244:106289. PMID: 41067565 -
Antiviral Res
First clinical description of letermovir resistance mutation in cytomegalovirus UL51 gene and potential impact on the terminase complex structure. [Abstract]2022 Aug:204:105361. PMID: 35690130 -
Antiviral Res
Artemisone demonstrates synergistic antiviral activity in combination with approved and experimental drugs active against human cytomegalovirus. [Abstract]2019 Dec;172:104639. PMID: 31654672 -
Antiviral Res
In vitro evaluation of current and novel antivirals in combination against human cytomegalovirus. [Abstract]2018 Oct:158:255-263. PMID: 30153445 -
Antiviral Res
Antiviral activity of maribavir in combination with other drugs active against human cytomegalovirus. [Abstract]2018 Sep:157:128-133. PMID: 30040968 -
Antiviral Res
A third component of the human cytomegalovirus terminase complex is involved in letermovir resistance. [Abstract]2017 Dec:148:1-4. PMID: 29107686 -
J Virol
Functional and structural insights into HCMV terminase accessory proteins pUL77 and pUL93. [Abstract]2025 Sep 16:e0117325. PMID: 40956108 -
J Virol
Inhibition of Human Cytomegalovirus pUL89 Terminase Subunit Blocks Virus Replication and Genome Cleavage. [Abstract]2017 Jan 18;91(3). pii: e02152-16. PMID: 27881652 -
Bioorg Med Chem
Inhibition of the hERG potassium ion channel by different non-nucleoside human cytomegalovirus polymerase antiviral inhibitor series and the exploration of variations on a pyrroloquinoline core to reduce cardiotoxicity potential. [Abstract]2023 May 1:85:117276. PMID: 37037115 -
PLoS One
Placental transfer of Letermovir & Maribavir in the ex vivo human cotyledon perfusion model. New perspectives for in utero treatment of congenital cytomegalovirus infection. [Abstract]2020 Apr 30;15(4):e0232140. PMID: 32353010 -
Microbiol Immunol
A two-step culture method utilizing secreted luciferase recombinant virus for detection of anti-cytomegalovirus compounds. [Abstract]2018 Oct;62(10):651-658. PMID: 30187945 -
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용액&용해도
DMSO : ≥ 100 mg/mL (174.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
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.
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
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Marschall M, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7. [Content Brief]
[2]. Goldner T, et al. The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93. [Content Brief]
[3]. Lischka P, et al. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. [Content Brief]
[4]. Wildum S, et al. In vitro drug combination studies of Letermovir (AIC246, MK-8228) with approved anti-human cytomegalovirus (HCMV) and anti-HIV compounds in inhibition of HCMV and HIV replication. Antimicrob Agents Chemother. 2015;59(6):3140-8. [Content Brief]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7466 mL | 8.7329 mL | 17.4657 mL | 43.6643 mL |
| 5 mM | 0.3493 mL | 1.7466 mL | 3.4931 mL | 8.7329 mL | |
| 10 mM | 0.1747 mL | 0.8733 mL | 1.7466 mL | 4.3664 mL | |
| 15 mM | 0.1164 mL | 0.5822 mL | 1.1644 mL | 2.9110 mL | |
| 20 mM | 0.0873 mL | 0.4366 mL | 0.8733 mL | 2.1832 mL | |
| 25 mM | 0.0699 mL | 0.3493 mL | 0.6986 mL | 1.7466 mL | |
| 30 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4555 mL | |
| 40 mM | 0.0437 mL | 0.2183 mL | 0.4366 mL | 1.0916 mL | |
| 50 mM | 0.0349 mL | 0.1747 mL | 0.3493 mL | 0.8733 mL | |
| 60 mM | 0.0291 mL | 0.1455 mL | 0.2911 mL | 0.7277 mL | |
| 80 mM | 0.0218 mL | 0.1092 mL | 0.2183 mL | 0.5458 mL | |
| 100 mM | 0.0175 mL | 0.0873 mL | 0.1747 mL | 0.4366 mL |
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