Valacyclovir hydrochloride

SKU: orb1226681

Description

An antiviral agent that acts as a very potent inhibitor of viral DNA polymerase; a prodrug of aciclovir for management of herpes simplex (HSV), herpes zoster and herpes B infection.HSV Infection Approved(In Vitro):Valacyclovir hydrochloride (Valaciclovir hydrochloride; VACV) uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 mM and 23.34 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro.(In Vivo):For treatment of a first episode of genital herpes, a large comparative trial has shown that Valacyclovir hydrochloride (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day.The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1,000 mg of valacyclovir three times a day.EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b.i.d., 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA.

Key Properties

• CAS Number: 124832-27-5
• MW: 360.7966
• Purity: >98% (HPLC)
• Formula: C₁₃H₂₁ClN₆O₄
• SMILES: CC(C)[C@@H](C(=O)OCCOCN1C=NC2=C1NC(=NC2=O)N)N.Cl
• Target: HSV
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  For treatment of a first episode of genital herpes, a large comparative trial has shown that Valacyclovir hydrochloride (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day. The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1, 000 mg of valacyclovir three times a day. EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b. i. d. , 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA.
• In Vitro:
  Valacyclovir hydrochloride (Valaciclovir hydrochloride; VACV) uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 mM and 23.34 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Valaciclovir hydrochloride

Quick Database Links

Gene Symbol

HSV