| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g | |||
| Other Sizes |
| Targets |
The active metabolite, ganciclovir, targets the CMV DNA polymerase. Ganciclovir is phosphorylated to ganciclovir triphosphate by viral protein kinases (UL97 in CMV) and then inhibits viral DNA synthesis by competing with deoxyguanosine triphosphate for incorporation into viral DNA, causing chain termination.
|
|---|---|
| ln Vitro |
In vitro, valganciclovir itself shows little activity; it is the active metabolite ganciclovir that inhibits CMV replication. Ganciclovir inhibits CMV DNA polymerase with an IC50 in the sub-micromolar range. It is active against human CMV and other herpesviruses.
|
| ln Vivo |
In vivo, valganciclovir is well absorbed after oral administration and rapidly hydrolyzed to ganciclovir. It reduces CMV viral load in infected patients. It is used for the prevention of CMV disease in transplant recipients and for the treatment of CMV retinitis in AIDS patients.
|
| Enzyme Assay |
In vitro antiviral assays are performed using CMV-infected human fibroblasts. Valganciclovir is added to the culture medium, and viral replication is assessed by plaque reduction assay or by measuring viral DNA load using qPCR. The EC50 for CMV inhibition is determined from dose-response curves.
|
| Cell Assay |
Cells (human foreskin fibroblasts) are cultured in 24-well plates and infected with CMV. After viral adsorption, cells are overlaid with medium containing various concentrations of valganciclovir. After 7-10 days, plaques are counted. Alternatively, viral DNA is extracted and quantified by qPCR. Cytotoxicity is assessed in parallel using uninfected cells.
|
| Animal Protocol |
Animal models for CMV include immunocompromised mice infected with murine CMV or human CMV xenograft models. Valganciclovir is administered orally or intraperitoneally. Viral titers in tissues (e.g., liver, spleen, salivary glands) are measured by plaque assay or qPCR. Survival and clinical signs are monitored.
|
| ADME/Pharmacokinetics |
Valganciclovir (as the HCl hydrate) is a prodrug with improved oral bioavailability (~60%) compared to ganciclovir (~5%). It is rapidly hydrolyzed to ganciclovir by intestinal and hepatic esterases. Ganciclovir has a half-life of 4-6 hours in patients with normal renal function and is excreted unchanged in the urine. Dose adjustment is required in renal impairment.
|
| Toxicity/Toxicokinetics |
Valganciclovir HCl hydrate has well-characterized toxicity. Common adverse effects include gastrointestinal disturbances (nausea, diarrhea), myelosuppression (neutropenia, anemia, thrombocytopenia), and headache. It is teratogenic and embryotoxic in animals. It is contraindicated in patients with severe hypersensitivity.
|
| References |
J Pharm Sci.2000 Jun;89(6):781-9;Drugs.2005;65(6):859-78.
|
| Additional Infomation |
Valganciclovir hydrochloride is an antiviral prescription drug approved by the U.S. Food and Drug Administration (FDA) for the treatment of cytomegalovirus retinitis (CMV retinitis) in adults with HIV/AIDS. Valganciclovir hydrochloride is also FDA-approved for the prevention of CMV infection in organ transplant recipients (who are at risk of CMV infection). CMV infection, including CMV retinitis, can be an opportunistic infection (OI) of HIV. Valganciclovir hydrochloride is the hydrochloride form of valganciclovir, a prodrug of ganciclovir, a 2'-deoxyguanosine nucleoside analog with antiviral activity. Upon phosphorylation, valganciclovir is incorporated into DNA, thereby inhibiting viral DNA polymerase and thus viral replication. Valganciclovir is a ganciclovir prodrug and antiviral drug used to treat cytomegalovirus retinitis in patients with HIV/AIDS and to prevent cytomegalovirus infection in patients who have received organ transplants from cytomegalovirus-positive donors. See also: valganciclovir (its salt form).
Valganciclovir is a clinically approved antiviral drug for CMV infections. It is available as oral tablets and solution. The recommended dose for CMV retinitis is 900 mg twice daily for 21 days. For CMV prophylaxis, the dose is 900 mg once daily. It was approved by the FDA in 2001. It is marketed under the brand name Valcyte. |
| 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)
|
| 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. View More
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. 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. |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
