| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
HSV-1 (IC50 = 2.9 μg/mL)
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|---|---|
| ln Vitro |
At concentrations of 1.64 mM and 23.34 nmol/mg protein/5 min, respectively, the maximal rates of valacyclovir hydrochloride (valaciclovir hydrochloride, VACV) uptake are concentration-dependent and saturable. The in vitro intestinal transport properties of VACV are dominated by hPEPT1, as demonstrated by the very identical Km values observed in hPEPT1/CHO cells, rat and rabbit tissues, and Caco-2 cells [5].
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| ln Vivo |
A major comparative trial found that valacyclovir hydrochloride (1 g twice daily) for 10 days was just as effective as acyclovir (200 mg 5 times daily) for treating a first bout of genital herpes. Two trials found that valacyclovir (200 mg five times daily) was equally efficacious as acyclovir (200 mg five times daily) in a five-day treatment cycle for managing relapses. Valacyclovir at a dose of 1 g per day works just as well as 2 g per day. One dose of valacyclovir can be given every day [1]. Serum and cerebrospinal fluid acyclovir concentrations were assessed at steady state following six days of oral valacyclovir 1,000 mg three times a day [2]. PE and AC have EC50 values in 3T3 cells of 0.02 and 0.01 ug/ml, however in BHK cells they are 0.2 and 0.03 ug/ml. Immunosuppressed mice that were infected were treated with FA and VA (bid, 5.5 days) to eradicate otoparesis, ear lesions (vesicles, etc.), and death. The percentage of erythema was also reduced from 100% to 24% and 38%. By day six, the virus had vanished from the ears and brainstem, but in mice receiving VA treatment, it returned when the medication was stopped [3].
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| Enzyme Assay |
The in vitro 50% inhibitory concentration (IC50) of HSV-1 W strain was determined by using a plaque-reduction assay to verify its sensitivity to acyclovir. The IC50 for HSV-1 W was determined to be 2.9 µg/ml. [4].
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| Animal Protocol |
Forty-seven NZW rabbits latently infected with HSV-1 W strain were divided into four groups: I, 50 mg/kg/day valacyclovir; II, 100 mg/kg/day valacyclovir; III, 150 mg/kg/day valacyclovir; and IV, saline control. One half of the total dose of valacyclovir was delivered via intraperitoneal injections twice daily for 7 days beginning with one dose before excimer laser keratectomy. HSV-1 ocular shedding was determined from eye cultures for 7 days after treatment.The administration of both 100 mg/kg/day (group II) and 150 mg/kg/day (group III) of valacyclovir significantly reduced the number of eyes from which latent HSV-1 was recovered compared with the control group. There was no difference between the control group and group I (50 mg/kg/day valacyclovir). However, all three valacyclovir dosages significantly reduced the total number of HSV-1 shedding days compared with the control group, and 100% HSV-1 TG latency was demonstrated for all four groups.[4]
The document summarizes clinical trial data and does not provide detailed protocols for animal studies. The reported trials were conducted in immunocompetent human patients. [1] * **Treatment of First Episode:** A randomized, double-blind study involving 643 patients. Treatment with valacyclovir (1 g twice a day) or acyclovir (200 mg five times a day) was initiated within 72 hours of lesion appearance and continued for 10 days. Intention-to-treat analysis was performed. [1] * **Treatment of Recurrences:** Patients were enrolled in double-blind trials. Treatment began within 24 hours of the onset of symptoms or recurrence. Various dosing regimens of valacyclovir were compared against acyclovir or placebo for a duration of 5 days. [1] * **Prevention of Recurrences:** A double-blind, placebo-controlled trial lasting 16 weeks. Patients with at least eight yearly episodes of genital herpes received either valacyclovir (500 mg once daily) or placebo. The primary endpoint was the proportion of patients remaining recurrence-free. [1] |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of use during lactation After valacyclovir administration, the acyclovir content in breast milk is less than 1% of the typical infant dose, and no adverse effects are expected on breastfed infants. No special precautions are required for the use of valacyclovir during lactation. One study showed that valacyclovir administration to mothers co-infected with herpes simplex virus type 2 and HIV reduced HIV shedding in breast milk at 6 and 14 weeks postpartum, but this effect was not observed thereafter. [1] In another study of HIV-positive mothers, valacyclovir did not reduce cytomegalovirus (CMV) shedding in breast milk or the risk of CMV infection in infants. [2] ◉ Effects on breastfed infants In a study of pregnant women co-infected with HIV and herpes simplex virus, the mothers received 300 mg of zidovudine daily from week 34 of pregnancy to 12 months postpartum and nevirapine at delivery. Half of the women (n = 74) received 500 mg valacyclovir orally twice daily from 34 weeks of gestation to 12 months postpartum. At 6 weeks postpartum, all infants who received acyclovir via breast milk had normal serum creatinine levels (<0.83 mg/dL). Except for one infant with an ALT level of 70.1 units/L, the median serum creatinine and alanine aminotransferase (ALT) levels and growth were not different from those of infants who had not been exposed to valacyclovir. Infants whose mothers received valacyclovir generally experienced similar adverse reactions to those in the placebo group, but the treated infants had a lower risk of eczema and thrush than the placebo group. [1][4] ◉ Effects on lactation and breast milk No relevant published information was found as of the revision date. |
| References |
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| Additional Infomation |
Valacyclovir hydrochloride is an organic molecular entity. Valacyclovir hydrochloride is an antiviral prescription drug approved by the U.S. Food and Drug Administration (FDA) for: treating and/or preventing certain types of herpes simplex virus (HSV) infection, including genital herpes (genital lesions) and cold sores (cold sores); reducing the risk of transmitting genital herpes to others; and treating varicella-zoster virus (VZV) infection, including chickenpox (primary varicella infection) and shingles (herpesvirus infection). HSV and VZV infections can be opportunistic infections (OIs) of HIV. Opportunistic infections are those that are more common or more severe in people with weakened immune systems (such as those infected with HIV) than in people with healthy immune systems. Valacyclovir hydrochloride is the hydrochloride salt of valacyclovir. Valacyclovir is a prodrug of acyclovir, which, after metabolism, inhibits viral DNA replication. It is used to treat herpes simplex and varicella-zoster virus infections, and can also be used to prevent human cytomegalovirus infection. Valacyclovir is a prodrug of acyclovir, used to treat skin and mucous membrane infections (including genital herpes) caused by herpes zoster and herpes simplex virus. See also: Acyclovir (containing the active fraction); Valacyclovir (containing the active fraction).
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| Molecular Formula |
C13H21CLN6O4
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|---|---|
| Molecular Weight |
360.799
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| Exact Mass |
360.131
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| Elemental Analysis |
C, 43.28; H, 5.87; Cl, 9.83; N, 23.29; O, 17.74
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| CAS # |
124832-27-5
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| Related CAS # |
Valacyclovir-d8 hydrochloride;1279033-32-7;Valacyclovir;124832-26-4;Valacyclovir-d4 hydrochloride;1331910-75-8;Valacyclovir hydrochloride hydrate;1218948-84-5; 124832-27-5 (HCl); 950189-66-9
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| PubChem CID |
135398741
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| Appearance |
Typically exists as white to off-white solids at room temperature
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| Density |
1.55g/cm3
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| Boiling Point |
588.4ºC at 760 mmHg
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| Melting Point |
170-172ºC
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| Flash Point |
309.7ºC
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| Vapour Pressure |
7.95E-14mmHg at 25°C
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| Index of Refraction |
1.673
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| LogP |
1.285
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
24
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| Complexity |
483
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| Defined Atom Stereocenter Count |
1
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| SMILES |
N[C@@H](C(C)C)C(OCCOCN1C=NC2=C1N=C(N)NC2=O)=O.Cl
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| InChi Key |
ZCDDBUOENGJMLV-QRPNPIFTSA-N
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| InChi Code |
InChI=1S/C13H20N6O4.ClH/c1-7(2)8(14)12(21)23-4-3-22-6-19-5-16-9-10(19)17-13(15)18-11(9)20;/h5,7-8H,3-4,6,14H2,1-2H3,(H3,15,17,18,20);1H/t8-;/m0./s1
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| Chemical Name |
2-[(2-amino-6-oxo-1H-purin-9-yl)methoxy]ethyl (2S)-2-amino-3-methylbutanoate;hydrochloride
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| Synonyms |
Zelitrex; 256U87; Vacyclovir; 256U; L-valyl ester; BW256U87; Valacyclovir Hydrochloride; Valtrex L-valylacyclovir; Valacyclovir HCl; Valtrex; Valaciclovir hydrochloride; Valaciclovir Hcl; 256U87 hydrochloride; BW-256U87;
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~277.16 mM)
DMSO : ~43.33 mg/mL (~120.09 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.93 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 (6.93 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 (6.93 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 (277.16 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 | 2.7716 mL | 13.8581 mL | 27.7162 mL | |
| 5 mM | 0.5543 mL | 2.7716 mL | 5.5432 mL | |
| 10 mM | 0.2772 mL | 1.3858 mL | 2.7716 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.
Randomized open label clinical trial directed to optimize the duration of empirical antimicrobial therapy in haematologic patients with febrile neutropenia
CTID: null
Phase: Phase 3 Status: Completed
Date: 2012-03-26
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