Letermovir (GMP) is the GMP grade of Letermovir (HY-15233). GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Letermovir (GMP) is an orally active CMV inhibitor. Letermovir (GMP) targets the CMV terminase complex rather than CMV DNA polymerase and exerts its antiviral activity. Letermovir (GMP) can be used in the study of CMV infection.
For research use only. We do not sell to patients.
- CAS No.: 917389-32-3
- Formula: C29H28F4N4O4
- Molecular Weight:572.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEL | EC50 |
0.0046 μM
Compound: Letermovir
|
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
|
[PMID: 26001344] |
| HEL 299 | CC50 |
63 μM
Compound: AIC246
|
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
|
[PMID: 20047911] |
| HEL 299 | EC50 |
0.0035 μM
Compound: AIC246
|
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
|
[PMID: 20047911] |
| HS27 | CC50 |
107 μM
Compound: AIC246
|
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
|
[PMID: 20047911] |
| HS27 | EC50 |
0.0056 μM
Compound: AIC246
|
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
|
[PMID: 20047911] |
| MRC5 | CC50 |
127 μM
Compound: AIC246
|
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
|
[PMID: 20047911] |
| MRC5 | EC50 |
0.0045 μM
Compound: AIC246
|
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
|
[PMID: 20047911] |
| NHDF | CC50 |
91 μM
Compound: AIC246
|
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
|
[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.
Chemical Information
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CAS No. 917389-32-3
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Molecular Weight 572.55
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Formula C29H28F4N4O4
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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 (GMP); MK-8228 (GMP)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. 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]
[2]. 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]
[3]. 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]
[4]. 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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