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Art. -Nr.: HY-15233G

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Letermovir (GMP)

(Synonyms: AIC246 (GMP); MK-8228 (GMP))

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.

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CAS. Nr.: 917389-32-3
Formel: C₂₉H₂₈F₄N₄O₄
Molecular Weight:572.55

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

Letermovir (GMP) Chemical Structure

CAS. Nr.: 917389-32-3

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	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]

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].

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

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].

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

Chemical Information

CAS. Nr. 917389-32-3
Molecular Weight 572.55
Formel C₂₉H₂₈F₄N₄O₄
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
Synonyms

AIC246 (GMP); MK-8228 (GMP)
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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