[CAS NO. 176161-24-3]  Maribavir

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PRODUCTS SPECIFICATIONS [176161-24-3]

Catalog
HY-16305
Brand
MCE
CAS
176161-24-3

DESCRIPTION [176161-24-3]

Overview

MDLMFCD00945570
Molecular Weight376.24
Molecular FormulaC15H19Cl2N3O4
SMILESClC1=C(Cl)C=C2C(N=C(NC(C)C)N2[C@@H]3[C@@H](O)[C@@H](O)[C@H](CO)O3)=C1

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


Summary

Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC 50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus ( EBV ).


IC50 & Target

HCMV [1]


In Vitro

Maribavir is a potent inhibitor of the autophosporylation of the wild type and all the major Ganciclovir (GCV) resistant UL97 mutants analysed with a mean IC 50 of 35 nM. The M460I mutation results in hypersensitivity to Maribavir with an IC 50 of 4.8 nM. A Maribavir resistant mutant of UL97 (L397R) is functionally compromised as both a Ganciclovir kinase and a protein kinase (~ 10% of wild type levels). Enzyme kinetic experiments demonstrate that Maribavir is a competitive inhibitor of ATP with a K i of 10 nM [1] . Maribavir (1263W94) inhibits viral replication in a dose-dependent manner, with IC 50 of 0.12±0.01 μM as measured by a multicycle DNA hybridization assay. The pUL97 protein kinase is strongly inhibited by Maribavir, with 50% inhibition occurring at 3 nM [2] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04131556 Shire|Takeda
Healthy Volunteers
October 25, 2019 Phase 1
NCT04497883 Shire|Takeda
Healthy Volunteers
August 7, 2020 Phase 1
NCT01611974 Shire|Takeda
Cytomegalovirus (CMV)
July 17, 2012 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


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 : 200 mg/mL ( 531.58 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6579 mL 13.2894 mL 26.5788 mL
5 mM 0.5316 mL 2.6579 mL 5.3158 mL
10 mM 0.2658 mL 1.3289 mL 2.6579 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

    Solubility: ≥ 2.87 mg/mL (7.63 mM); Clear solution

  • 2.

    Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.87 mg/mL (7.63 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

  • 5.

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

    Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

1H-Benzimidazol-2-amine, 5,6-dichloro-N-(1-methylethyl)-1-β-L-ribofuranosyl-
5,6-Dichloro-N-(1-methylethyl)-1-β-L-ribofuranosyl-1H-benzimidazol-2-amine
BW 1263W94
1263W94
Maribavir
GW 257406X