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伐昔洛韋

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names：
Valacyclovir
CAS號：
124832-26-4
MDL Number： MFCD00866955
MF(分子式)： C13H20N6O4 MW(分子量)： 324.34
EINECS:1312995-182-4 Reaxys Number:
Pubchem ID:135398742 Brand:BIOFOUNT

伐昔洛韋(124832-26-4,Valacyclovir)是一種抗病毒藥物，用于治療單純皰疹，帶狀皰疹和B型皰疹。IC50值：2.9微克/毫升（對于HSV-1 W）[4]。；目標(biāo)：HSV感染；體外：VACV的攝取是濃度依賴性的并且可飽和，其Michaelis-Menten常數(shù)和最大速度分別為1.64 +/- 0.06 mM和23.34 +/- 0.36 nmol / mg蛋白/ 5 min。在hPEPT1 / CHO細(xì)胞，大鼠和兔子組織以及Caco-2細(xì)胞中獲得了非常相似的Km值，這表明hPEPT1在體外VACV的腸道轉(zhuǎn)運特性中占主導(dǎo)地位.

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM000721-50mg	50mg		￥ 706.00	￥ 706.00		Backorder	- +	￥ 0.00
YZM000721-10mg	10mg	>97%	￥ 438.75	￥ 438.75		2-3天	- +	￥ 0.00

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中文別名	伐昔洛韋(124832-26-4);青霉素G鹽-D7;萬乃洛韋;L-纈氨酸2-（（2-氨基-1,6-二氫-6-氧代-9H-嘌呤-9-基）甲氧基）乙基;256U87;阿昔洛韋，L戊酯;阿昔洛韋，L-戊酸酯;BW256U87;D-伐昔洛韋;纈氨昔洛韋;L-戊酸酯阿昔洛韋;鹽酸伐昔洛韋;鹽酸伐昔洛韋（DL）-異構(gòu)體;伐昔洛韋（D）-異構(gòu)體;伐昔洛韋（DL）-異構(gòu)體;伐昔洛韋（L）-異構(gòu)體;伐昔洛韋，D-;伐昔洛韋，鹽酸x，（D）-異構(gòu)體;伐昔洛韋，x-鹽酸鹽，（DL）-異構(gòu)體;瓦爾特雷克斯;
英文別名	Valacyclovir(124832-26-4);2-((2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy)ethyl L-valinate;256U87;Acyclovir, L valyl Ester;acyclovir, L-valyl ester;BW256U87;D- Valacyclovir;L Valylacyclovir;L-valyl Ester Acyclovir;L-valylacyclovir;valaciclovir;valacyclovir;valacyclovir hydrochloride;valacyclovir hydrochloride, (DL)-isomer;valacyclovir, (D)-isomer;valacyclovir, (DL)-isomer;valacyclovir, (L)-isomer;Valacyclovir, D-;valacyclovir, x-hydrochloride, (D)-isomer;valacyclovir, x-hydrochloride, (DL)-isomer;Valtrex;
CAS號	124832-26-4
Inchi	InChI = 1S / C13H20N6O4 / 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）/ t8- / m0 / s1
InchiKey	HDOVUKNUBWVHOX-QMMMGPOBSA-N
分子式 Formula	C13H20N6O4
分子量 Molecular Weight	324.34
溶解度Solubility
性狀	白色至灰白色結(jié)晶粉末
儲藏條件 Storage conditions	請根據(jù)產(chǎn)品建議的存儲條件進行存儲,Please store the product under the recommended condition sin the description.

伐昔洛韋(124832-26-4,Valacyclovir)毒理性質(zhì)：
Oral therapy with valacyclovir is associated with a low rate of mild-to-moderate serum aminotransferase elevations, but these abnormalities are usually asymptomatic and self-limited even with continuation of therapy. Complicating the attribution of liver test abnormalities to valacyclovir therapy is the fact that enzyme elevations are not uncommon during the course of varicella-zoster infection (shingles) and can progress to clinically apparent hepatitis and even acute liver failure. Clinically apparent liver disease due to valacyclovir itself is rare, but isolated reports have been published. The time to onset was short (1 to 2 weeks) and the course mild, with few symptoms and rapid resolution (Case 1). The pattern of liver injury described was mixed hepatocellular-cholestatic. Immunoallergic features and autoantibodies were absent.

伐昔洛韋(124832-26-4,Valacyclovir)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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產(chǎn)品說明	伐昔洛韋(124832-26-4,Valacyclovir)是抗病毒化合物，對HSV-1 W的IC50為2.9μg/ ml。
Introduction	伐昔洛韋(124832-26-4,Valacyclovir)is an antiviral drug used in the management of herpes simplex, herpes zoster, and herpes B. IC50 Value: 2.9 microg/ml (for HSV W)[4].
Application1	Valaciclovir是一種抗病毒藥物，用于治療單純皰疹，帶狀皰疹和B型皰疹。
Application2	伐昔洛韋是阿昔洛韋的左旋纈氨酸酯,是阿昔洛韋的前體藥物。用于治療水痘、帶狀皰疹及Ⅰ型、Ⅱ型單純皰疹的感染,包括初發(fā)和復(fù)發(fā)的生殖器皰疹。
Application3

伐昔洛韋(124832-26-4,Valacyclovir)藥理學(xué)：

1、伐昔洛韋是一種抗病毒藥物，伐昔洛韋用于治療單純皰疹，帶狀皰疹和B型皰疹。

2、伐昔洛韋是抗病毒藥物阿昔洛韋的L-戊酸酯的鹽酸鹽?？诜o藥時，伐昔洛韋迅速轉(zhuǎn)化為無環(huán)鳥苷，其經(jīng)過進一步轉(zhuǎn)化為核苷酸類似物抑制病毒DNA復(fù)制阿昔洛韋三磷酸通過病毒胸苷激酶，細(xì)胞脒環(huán)化酶，以及許多其他細(xì)胞酶。三磷酸阿昔洛韋競爭性抑制病毒DNA聚合酶；整合并終止正在增長的病毒DNA鏈；并滅活病毒DNA聚合酶。阿昔洛韋的抗病毒活性更高與水痘帶狀皰疹病毒（VZV）相比，抗單純皰疹病毒（HSV）的原因在于其可被HSV 胸苷激酶更有效地磷酸化。

3、伐昔洛韋是無環(huán)鳥苷的核苷類似物抗病毒劑和前藥，用于治療皰疹和水痘-帶狀皰疹病毒感染。伐昔洛韋與罕見的輕度，臨床上明顯的肝損傷有關(guān)。

4、伐昔洛韋是L-戊酸酯。它具有抗病毒藥的作用。它來自鳥嘌呤。

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

伐昔洛韋(124832-26-4,Valacyclovir)危害標(biāo)識：

象形圖
信號	Warning
GHS危險說明	The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
GHS危險說明	H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
防范說明代碼	P264, P270, P301+P312, P330, and P501
防范說明代碼	(The corresponding statement to each P-code can be found at the GHS Classification page.)

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

Lycke J, Malmestr?m C, St hle L. Acyclovir levels in serum and cerebrospinal fluid after oral administration of valacyclovir. Antimicrob Agents Chemother. 2003 Aug;47(8):2438-41.

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.

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.

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

伐昔洛韋(124832-26-4,Valacyclovir)參考文獻(xiàn)：

1. Carbon nanotube based electrochemical sensor for the sensitive detection of valacyclovir
Badal Shah, Todd La?eur and Aicheng Chen*. Faraday Discuss., 2013, 164, 135–146

Substituted purines represent an important category of compounds that are actively used as therapeutic agents against viral infection. Valacyclovir is the drug of choice for the treatment of herpes zoster and cold sores. It is also e?ective for the treatment or suppression of genital herpes in immunocompetent individuals and for the suppression of recurrent genital herpes in HIV infected individuals. The chemical structure of valacyclovir is shown in Scheme 1. Valacyclovir is the L-valyl ester and prodrug of the antiviral drug acyclovir. Subsequent to absorption, valacyclovir is rapidly and almost completely hydrolyzed to acyclovir and L-valine, an essential amino acid, via first-pass metabolism. This hydrolysis is mediated primarily by the enzyme valacyclovir hydrolase and occurs predominantly in the liver. Because of the low bioavailability of acyclovir, its prodrug (valacyclovir) is preferred for therapeutic treatment, through which it plays an important role in the therapy of viral diseases. This drug provides significant therapeutic benefits in the treatment of viral diseases, and no serious side e?ects associated with its use have been reported in its monograph. Because of the wide use of valacyclovir in the treatment of di?erent viral diseases, its quantitative analysis has become very important and is under extensive study.

2. Spectro?uorimetric and TLC-densitometric methods for a stability indicating assay of valacyclovir hydrochloride in the presence of its degradation product
Sayed M. Derayea, Islam M. Mostafa and Mahmoud A. Omar*. RSC Adv.,2014, 4,42308–42315

Valacyclovir hydrochloride (VAC) is L-valine 2-[(2-amino-1,6-dihy-dro-6-oxo-9H-purin-9yl)methoxy]ethyl ester hydrochloride (Fig. 1). After its oral administration, VAC is rapidly converted into acyclovir which has demonstrated antiviral activity, against herpes simple xvirus type I (HSV-1),type 2 (HSV-II) and Varicella zoster virus. The oral bioavailability of acyclovir is higher after administration of VAC relative to acyclovir itself. The mechanism of action of acyclovir involves the highly selective inhibition of virus DNA replication, via enhanced uptake in virus-infected cells and phosphorylation by viral thymidine kinase. Few analytical methods have been reported for the determination of VAC. These methods include: spectrophotometric, chromatographic, capillary electrophoretic and electrochemical methods. To the present time there is no spectrofluorometric method reported for analysis of VAC. Accordingly we here present the first attempt for spectrofluorimetric method in addition to TLC-densitometry for the determination of VAC in pure form and pharmaceutical tablets.

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