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124832-27-5

124832-27-5 structure
124832-27-5 structure
  • Name: Valacyclovir hydrochloride
  • Chemical Name: Valacyclovir Hydrochloride Hydrate
  • CAS Number: 124832-27-5
  • Molecular Formula: C13H21ClN6O4
  • Molecular Weight: 360.797
  • Catalog: API Synthetic anti-infective drugs Antiviral drugs
  • Create Date: 2018-02-03 08:00:00
  • Modify Date: 2024-01-01 21:32:41
  • Valacyclovir hydrochloride is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. Target: HSVValacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. VACV uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 +/- 0.06 mM and 23.34 +/- 0.36 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 . For treatment of a first episode of genital herpes, a large comparative trial has shown that valacyclovir (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.

Name Valacyclovir Hydrochloride Hydrate
Synonyms 2-((2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy)ethyl ester monohydrochloride
MFCD01861507
2-[(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl L-valinate hydrochloride
L-Valine 2-(2-Amino-1,6-dihydro-6-oxo-9H-purin-9-ylmethoxy)ethyl Ester Hydrochloride Hydrate
Valaciclovir
2-[(2-Amino-6-oxo-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl valinate hydrochloride (1:1)
2-[(2-Amino-6-oxo-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl-(2S)-2-amino-3-methylbutanoathydrochlorid
2-[(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)methoxy]ethyl (2S)-2-amino-3-methylbutanoate hydrochloride
Valacyclovir hydrochloride
Zelitrex
Valaciclovir hydrochloride
(2S)-2-amino-3-méthylbutanoate de 2-[(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)méthoxy]éthyle chlorhydrate
Valaciclovir HCl
256u
L-Valine 2-((2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy)ethyl ester monohydrochloride
Valine, 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]ethyl ester, hydrochloride (1:1)
Valacyclovir hydrochloride hydrate
Valacyclovir (hydrochloride)
Description Valacyclovir hydrochloride is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. Target: HSVValacyclovir is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. VACV uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 +/- 0.06 mM and 23.34 +/- 0.36 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 . For treatment of a first episode of genital herpes, a large comparative trial has shown that valacyclovir (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.
Related Catalog
References

[1]. Valacyclovir. New indication: for genital herpes, simpler administration. Can Fam Physician. 1999 Jul;45:1698-700, 1703-5.

[2]. Lycke J, et al. Acyclovir levels in serum and cerebrospinal fluid after oral administration of valacyclovir. Antimicrob Agents Chemother. 2003 Aug;47(8):2438-41.

[3]. Comparison of efficacies of famciclovir and valaciclovir against herpes simplex virus type 1 in a murineimmunosuppression model. Antimicrob Agents Chemother. 1995 May;39(5):1114-9.

[4]. Dhaliwal DK, Romanowski EG, Yates KA, Valacyclovir inhibits recovery of ocular HSV-1 after experimental reactivation by excimer laser keratectomy. Cornea. 1999 Nov;18(6):693-9.

[5]. Guo A, Hu P, Balimane PV, Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.J Pharmacol Exp Ther. 1999 Apr;289(1):448-54.

Density 1.55g/cm3
Boiling Point 588.4ºC at 760 mmHg
Melting Point 170-172ºC
Molecular Formula C13H21ClN6O4
Molecular Weight 360.797
Flash Point 309.7ºC
Exact Mass 360.131287
PSA 151.14000
LogP 1.28590
Vapour Pressure 7.95E-14mmHg at 25°C
Index of Refraction 1.673
Storage condition Refrigerator
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Hazard Codes Xi: Irritant;
Risk Phrases R36/37/38
Safety Phrases 26-36
RIDADR NONH for all modes of transport
HS Code 2933990090
HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%