[CAS NO. 175865-59-5]  Valganciclovirhydrochloride

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PRODUCTS SPECIFICATIONS [175865-59-5]

Catalog
HY-A0032A
Brand
MCE
CAS
175865-59-5

DESCRIPTION [175865-59-5]

Overview

MDLMFCD08460118
Molecular Weight390.82
Molecular FormulaC14H23ClN6O5
SMILESN[C@@H](C(C)C)C(OCC(OCN1C=NC2=C1N=C(N)NC2=O)CO)=O.[H]Cl

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

Summary

Valganciclovir (hydrochloride), the L-valyl ester of ganciclovir, is actually a prodrug for ganciclovir. Valganciclovir is an antiviral medication used to treat cytomegalovirus infections. IC50 Value: Target: CMV in vitro: In cell culture model systems using Caco-2 cells for PEPT1 and SKPT cells for PEPT2, valganciclovir inhibited glycylsarcosine transport mediated by PEPT1 and PEPT2 with K(i) values (inhibition constant) of 1.68+/-0.30 and 0.043+/- 0.005 mM, respectively. The inhibition by valganciclovir was competitive in both cases [1]. in vivo: 37 patients were enrolled; 19 patients received treatment with VGV and 18 patients received treatment with GCV. The VGV was not inferior in efficacy to GCV as pre-emptive therapy, with rates of viral clearance at 28 days of 89.5% and 83%, respectively (P-value for non-inferiority = 0.030). Toxicities were similar between the 2 arms. No patients developed CMV disease [2]. Patients being treated with an alemtuzumab-containing regimen received prophylaxis with either valaciclovir 500 mg orally daily orvalganciclovir 450 mg orally twice daily. None of the 20 patients randomized to valganciclovir experienced CMV reactivation (P = .004) [3].


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00031434 National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Infections
July 2002 Phase 1|Phase 2
NCT00017784 Hoffmann-La Roche|NIH AIDS Clinical Trials Information Service
Cytomegalovirus Retinitis|HIV Infections
Phase 3
NCT00006145 National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Infections|HIV Infections
August 2000 Phase 3

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)


Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 127.94 mM ; Need ultrasonic)

H 2 O : ≥ 50 mg/mL ( 127.94 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5587 mL 12.7936 mL 25.5872 mL
5 mM 0.5117 mL 2.5587 mL 5.1174 mL
10 mM 0.2559 mL 1.2794 mL 2.5587 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 100 mg/mL (255.87 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

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


Synonyms

L-Valine, 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester, hydrochloride (1:1)
L-Valine, 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester, monohydrochloride
RS 079070-194
Valganciclovir hydrochloride
Ro 107-9070/194
Valcyte