GLPBio

Maribavir

Catalog No.: GC10390Purity:>98.00%Synonyms: 1263W94; BW1263W94; GW257406X
COASDSData Sheet
Maribavir is an orally active benzimidazole riboside antiviral agent. Maribavir competitively inhibits CMV pUL97 kinase activity (IC50=3nM).

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Maribavir
Cas No.: 176161-24-3
10mM (in 1mL DMSO)In Stock
$122.00
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1mgIn Stock
$52.00
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5mgIn Stock
$111.00
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10mgIn Stock
$179.00
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25mgIn Stock
$322.00
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50mgIn Stock
$447.00
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100mgIn Stock
$620.00
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200mgIn Stock
$853.00
1
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Description

Maribavir is an orally active benzimidazole riboside antiviral agent. Maribavir competitively inhibits CMV pUL97 kinase activity (IC50=3nM). Maribavir blocks viral DNA replication, capsid formation, and nuclear egress. Maribavir retains activity against some traditional anti-CMV drug-resistant strains. Maribavir is used for refractory/resistant cytomegalovirus infection after transplantation and related research[1-4].

In vitro, human embryonic lung fibroblasts were treated with 0-100μM maribavir for 0-16 days. Maribavir inhibited cytomegalovirus replication yield measured by reporter gene SEAP expression[5]. MRC-5 cells infected with human cytomegalovirus were treated with 0.1-40μM maribavir for 24-96 hours. Maribavir reduced viral DNA accumulation and decreased viral titers[6]. Human foreskin fibroblasts were treated with 1-7μM maribavir for 6 days. Maribavir inhibited human cytomegalovirus AD169 strain replication[7].

In vivo, Sprague-Dawley rats were orally administered 0-400mg/kg/day Maribavir once daily for 1 month. Maribavir caused neutrophilia, increased lymphocyte, monocyte and total WBC counts, mild elevated bilirubin, increased absolute and relative adrenal, liver and spleen weights, and mild reversible intestinal mucosal hyperplasia[8].

References:
[1] Levien TL, Baker DE. Maribavir. Hosp Pharm. 2023 Aug;58(4):336-344. doi: 10.1177/00185787221101480.
[2] Kang C. Maribavir: First Approval. Drugs. 2022 Feb;82(3):335-340.
[3] Sun K, Fournier M, Sundberg AK, et al. Maribavir: Mechanism of action, clinical, and translational science. Clin Transl Sci. 2024 Jan;17(1):e13696.
[4] Razonable RR. Current Perspectives on Letermovir and Maribavir for the Management of Cytomegalovirus Infection in Solid Organ Transplant Recipients. Drug Des Devel Ther. 2024 Sep 6;18:3987-4001.
[5] Chou S, Van Wechel L C, Marousek G I. Effect of cell culture conditions on the anticytomegalovirus activity of maribavir. Antimicrob Agents Chemother. 2006 Jul;50(7):2557-2559.
[6] Reitsma J, Terhune S, et al. Inhibition of cellular STAT3 synergizes with the cytomegalovirus kinase inhibitor maribavir to disrupt infection. Antiviral Res. 2014;104:74-85.
[7] Williams S L, Hartline C B, Kushner N L, et al. In vitro activities of benzimidazole D- and L-ribonucleosides against herpesviruses. Antimicrob Agents Chemother. 2003 Jul;47(7):2186-2192.
[8] Koszalka G W, Johnson N W, Good S S, et al. Preclinical and toxicology studies of 1263W94, a potent and selective inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother. 2002 Aug;46(8):2373-80.

Protocol

Cell experiment [1]:

Cell lines

 MRC-5 fibroblasts (human lung fibroblast), ARPE-19 cells (human retinal pigment epithelial), U-373 cells (human astrocytoma)

Preparation Method

 MRC-5, ARPE-19 and U-373 cells were grown to confluence, starved in 0.5% FBS for 2 days, then infected with human cytomegalovirus and treated with 0.1-40μM Maribavir at time of infection, with compound renewed every 24h; viral DNA was measured by qPCR, viral titers by infectious units/plaque assay, proteins by Western blot, and viability by flow cytometry.

Reaction Conditions

 0.1-40μM; 24-96h

Applications

 Maribavir reduced human cytomegalovirus DNA accumulation and viral titers, inhibited pUL97 kinase activity, and together with STAT3 inhibitor S3i-201 caused cleaved caspase-3 and cleaved PARP in infected cells and loss of infected but not uninfected cells.
Animal experiment [2]:

Animal models

 Sprague-Dawley rats

Preparation Method

Rats were orally administered Maribavir at doses of 0-400mg/kg/day via gavage for 28 days. Satellite groups were used for toxicokinetics, reversibility, and histopathology.

Dosage form

0-400mg/kg/day; p.o.; 28 days

Applications

Maribavir caused dose-related reversible increases in neutrophils, lymphocytes, monocytes, and total WBC counts at ≥100mg/kg/day, mild reversible elevations in bilirubin in females at 200 and 400mg/kg/day, increases in absolute and relative adrenal, liver, and spleen weights, and minimal reversible intestinal mucosal hyperplasia at all doses.
References:
[1] Reitsma J M, Terhune S S. Inhibition of cellular STAT3 synergizes with the cytomegalovirus kinase inhibitor maribavir to disrupt infection. Antiviral Res. 2014;104:74-85.
[2] Koszalka G W, Johnson N W, Good S S, et al. Preclinical and toxicology studies of 1263W94, a potent and selective inhibitor of human cytomegalovirus replication. Antimicrob Agents Chemother. 2002 Aug;46(8):2373-80.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
176161-24-3
Synonyms
1263W94; BW1263W94; GW257406X
Chemical Name
(2S,3S,4R,5S)-2-((E)-5,6-dichloro-2-(isopropylimino)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol
SMILES
CC(/N=C1NC2=C(N\1[C@]3([H])[C@](O)([H])[C@](O)([H])[C@](O3)([H])CO)C=C(Cl)C(Cl)=C2)C
Molecular Formula
C15H19Cl2N3O4
Molecular Weight
376.24
Solubility
DMSO : 200 mg/mL (531.58 mM; Need ultrasonic)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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