Valganciclovir HCl hydrate is the L-valyl ester prodrug of ganciclovir which is an antiviral drug used to treat cytomegalovirus infections. Valganciclovir is an antiviral medication used to treat cytomegalovirus infections. Valganciclovir hydrochloride is a hydrochloride salt of the L-valyl ester of ganciclovir that exists as a mixture of two diastereomers. After administration, these diastereomers are rapidly converted to ganciclovir by hepatic and intestinal esterases. In cytomegalovirus (CMV)-infected cells, ganciclovir is initially phosphorylated to the monophosphate form by viral protein kinase, then it is further phosphorylated via cellular kinases to produce the triphosphate form. This triphosphate form is slowly metabolized intracellularly. The phosphorylation is dependent upon the viral kinase and occurs preferentially in virus-infected cells.
Physicochemical Properties
| Molecular Formula | C14H23CLN6O5 |
| Molecular Weight | 390.8226 |
| Exact Mass | 390.141 |
| CAS # | 175865-59-5 |
| Related CAS # | Valganciclovir;175865-60-8;Valganciclovir-d8 hydrochloride;1132088-63-1 |
| PubChem CID | 135413534 |
| Appearance | White to off-white solid powder |
| Boiling Point | 629.1ºC at 760 mmHg |
| Vapour Pressure | 1.08E-16mmHg at 25°C |
| LogP | 0.646 |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 9 |
| Heavy Atom Count | 26 |
| Complexity | 528 |
| Defined Atom Stereocenter Count | 1 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| References | J Pharm Sci.2000 Jun;89(6):781-9;Drugs.2005;65(6):859-78. |
| Additional Infomation |
Valganciclovir hydrochloride is an antiviral prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of cytomegalovirus retinitis (CMV retinitis) in adults with AIDS. Valganciclovir hydrochlorideis also FDA-approved for the prevention of CMV disease in recipients of organ transplants who are at risk for CMV diseases. CMV diseases, including CMV retinitis, can be opportunistic infections(OIs) of HIV. Valganciclovir Hydrochloride is a hydrochloride salt form of valganciclovir, a prodrug form of ganciclovir, a nucleoside analog of 2'-deoxyguanosine, with antiviral activity. After phosphorylation, valganciclovir is incorporated into DNA, resulting in inhibition of viral DNA polymerase, and viral replication. A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor. See also: Valganciclovir (is salt form of). |
Solubility Data
| Solubility (In Vitro) |
H2O : ≥ 50 mg/mL (~127.94 mM) DMSO : ~50 mg/mL (~127.94 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: 100 mg/mL (255.87 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |