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噴昔洛韋

NMR下載 COA and HPLC MSDS下載
names：
Penciclovir
CAS號：
39809-25-1
MDL Number： MFCD00866931
MF(分子式)： C10H15N5O3 MW(分子量)： 253.26
EINECS:663-371-3 Reaxys Number:
Pubchem ID:135398748 Brand:BIOFOUNT

噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)是一種新型的無環(huán)核苷類似物，已顯示出抗1型和2型HSV的功效，并且由于其活性形式在HSV感染的細胞中具有延長的半衰期，因此似乎具有藥理學優(yōu)勢。IC50值：2.3。0.8 mg / ml（EC50，抑制EBV DNA合成）；> 100mg / ml（P3HR-1和Raji細胞的細胞生長抑制濃度均為50％）；目標：HSV；體外：GCV或PCV處理可誘導S期細胞快速積聚并導致凋亡，GCV （和較小程度的PCV）增加磷脂酰絲氨酸轉(zhuǎn)運，誘導TUNEL陽性結(jié)果，細胞形態(tài)發(fā)生改變，引起碘化丙啶染色明顯，并引起DNA梯形化。用噴昔洛韋或阿昔洛韋分別以1和10 ug / ml處理B-95-8細胞7天。在1 ug / ml時，兩種化合物均無活性。

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 (￥)
YZM000713-100mg	100mg	>98.0%	￥ 1113.00	￥ 1113.00		2-3天	- +	￥ 0.00
YZM000713-50mg	50mg	>98.0%	￥ 696.15	￥ 696.15		2-3天	- +	￥ 0.00

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中文別名	噴昔洛韋(39809-25-1);9-（4-羥基-3-羥甲基丁-1-基）鳥嘌呤;西雷亞爾39123;RL-39123;那佛;昔洛韋;昔洛韋，鈉鹽;昔洛韋，一鈉鹽，一水合物;克塔韋爾;
英文別名	Penciclovir(39809-25-1); BRL-39123; BRL 39123; BRL39123; VSA 671; VSA671; VSA-671; Penciclovir; Denavir, Vectavir and Fenivir;9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine;RL 39123;RL-39123;enavir;enciclovir;enciclovir Visfarm;enciclovir, monosodium salt;enciclovir, monosodium salt, monohydrate;ectavir;
CAS號	39809-25-1
Inchi	InChI = 1S / C10H15N5O3 / c11-10-13-8-7（9（18）14-10）12-5-15（8）2-1-6（3-16）4-17 / h5-6， 16-17H，1-4H2，（H3,11,13,14,18）
InchiKey	JNTOCHDNEULJHD-UHFFFAOYSA-N
分子式 Formula	C10H15N5O3
分子量 Molecular Weight	253.26
溶解度Solubility	生物體外In Vitro:DMSO溶解度25 mg/mL(98.71 mM;Need ultrasonic)
性狀	白色結(jié)晶固體粉末,Power
儲藏條件 Storage conditions	-20°C Freezer， 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)毒理性質(zhì)：

Symptoms of overdose include headache, abdominal pain, increased serum lipase, nausea, dyspepsia, dizziness, and hyperbilirubinemia.

Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention.

Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination。

Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam . Use proparacaine hydrochloride to assist eye irrigation .

噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)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	噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)是抗病毒劑用于治療多種皰疹病毒感染.具有毒性低,
Introduction	噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)is reported to be potent againstHSVtypes 1 and 2 withIC50of 0.04.8 μg/mL and 0.06.4 μg/mL, respectively.
Application1	Penciclovir有效作用于HSV 1和2，IC50 分別為0.04-1.8μg/ mL和0.06-4.4μg/ mL。
Application2	噴昔洛韋是一種鳥苷類似物抗病毒藥物，用于治療各種皰疹病毒感染。它是一種核苷類似物，具有低毒性和良好的選擇性。
Application3

噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)藥理學：

※噴昔洛韋是一種具有抗病毒活性的合成無環(huán)鳥嘌呤衍生物，主要用于治療1型和2型單純皰疹病毒（HSV）的感染。在被HSV感染的細胞中，噴昔洛韋被病毒胸苷激酶磷酸化，隨后被細胞激酶轉(zhuǎn)化為活性代謝產(chǎn)物，噴昔洛韋三磷酸，通過阻斷脫氧鳥苷三磷酸底物的結(jié)合，競爭性抑制病毒HSV聚合酶。結(jié)果，選擇性抑制了皰疹病毒DNA的合成和復制。

※噴昔洛韋，也稱為地那韋或PCV，屬于被稱為次黃嘌呤的有機化合物。次黃嘌呤是含有嘌呤衍生物1H-purin-6（9H）-1的化合物。嘌呤是一個的由二環(huán)芳香族化合物嘧啶稠合至環(huán)的咪唑環(huán)。噴昔洛韋是一種藥物，用于治療因各種皰疹病毒感染而在嘴唇和面部反復發(fā)作的唇皰疹。噴昔洛韋以固體存在，微溶（在水中）和弱酸性化合物（基于其pKa）。已在多種生物流體（如尿液和血液）中檢測到噴昔洛韋。在細胞內(nèi)，噴昔洛韋主要位于細胞質(zhì)中。噴昔洛韋可以由鳥嘌呤生物合成。

※噴昔洛韋是鳥嘌呤的2-氨基嘌呤類成員，其中第9位的氫被4-羥基-3-（羥甲基）丁-1-基取代。一種抗病毒藥，局部給藥以治療唇皰疹。前藥泛昔洛韋用于口服給藥。它具有抗病毒藥的作用。它是2-氨基嘌呤的成員和丙烷-1,3-二醇的成員。它來自鳥嘌呤。

※噴昔洛韋（Penciclovir）是鳥嘌呤類似物類抗病毒藥物，用于治療多種皰疹病毒感染。具有毒性低，病毒敏感性高等特點。噴昔洛韋口服吸收低，常用于局部給藥。泛昔洛韋是噴昔洛韋的前藥，口服吸收好。

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

噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)危害標識：

象形圖
信號	Warning
GHS危險說明	H319 (100%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]
GHS危險說明	Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范說明代碼	P264, P280, P305+P351+P338, and P337+P313
防范說明代碼	(The corresponding statement to each P-code can be found at the GHS Classification page.)

Piret J, et al. Resistance of herpes simplex viruses to nucleoside analogues: mechanisms, prevalence, and management. Antimicrob Agents Chemother. 2011 Feb;55(2):459-72.

Xiong Z, et al. Imaging chemically modified adenovirus for targeting tumors expressing integrin alphavbeta3 in living micewith mutant herpes simplex virus type 1 thymidine kinase PET reporter gene. J

Antiviral Consideration for Transplantation Including Drug Resistance Principles and Practice of Transplant Infectious Diseases 2019

Phenotypic and Genotypic Testing of HSV-1 and HSV-2 Resistance to Antivirals Herpes Simplex Virus 2020 31617182

Pharmacokinetics and Pharmacodynamics of Antiviral Drugs in Special Population Principles and Practice of Transplant Infectious Diseases 2019

噴昔洛韋(39809-25-1,Penciclovir,BRL 39123,VSA 671)參考文獻：

1.Clinical and antiviral effect of a single oral dose of famciclovir administered to cats at intake to a shelter.
Litster AL1, Lohr BR2, Bukowy RA2, Thomasy SM3, Maggs DJ3. Vet J. 2015 Feb;203(2):199-204. doi: 10.1016/j.tvjl.2014.11.011. Epub 2014 Nov 25.

Although famciclovir is efficacious in feline herpesvirus type 1 (FHV-1)-infected cats, effects of a single dose early in disease course have not been reported. In this two part, randomized, masked, placebo controlled study, cats received a single dose of 125 mg famciclovir (n = 43) or placebo (n = 43; pilot study), or 500 mg famciclovir (n = 41) or placebo (n = 40; clinical trial) on entering a shelter. FHV-1 PCR testing was performed, bodyweight and food intake were recorded, and signs of respiratory disease were scored prior to and 7 days following treatment. FHV-1 DNA was detected in 40% of cats in both parts at study entry. In the pilot study, ocular and nasal discharge scores increased from days 1 to 7 in famciclovir and placebo treated cats. Sneezing scores increased and bodyweight decreased in famciclovir-treated cats. The proportion of cats in which FHV-1 DNA was detected increased over time in all cats in the pilot study. In the clinical trial, food intake and median clinical disease scores for nasal discharge and sneezing increased from days 1 to 7 in both groups and demeanor scores worsened in famciclovir-treated cats.

2.Ribavirin inhibits human parainfluenza virus type 2 replication in vitro.
Kihira S1, Uematsu J, Kawano M, Itoh A, Ookohchi A, Satoh S, Maeda Y, Sakai K, Yamamoto H, Tsurudome M, O'Brien M, Komada H. Microbiol Immunol. 2014 Nov;58(11):628-35. doi: 10.1111/1348-0421.12192.

The antiviral activities of eight nucleoside analog antiviral drugs (ribavirin, acyclovir, lamivudine, 3'-azido-3'-deoxythymidine, emtricitabine, tenofovir, penciclovir and ganciclovir) against human parainfluenza virus type 2 (hPIV-2) were investigated. Only ribavirin (RBV) inhibited both cell fusion and hemadsorption induced by hPIV-2. RBV considerably reduced the number of viruses released from the cells. Virus genome synthesis was inhibited by RBV, as determined by real time PCR. An indirect immunofluorescence study showed that RBV largely inhibited viral protein synthesis. mRNAs of the proteins were not detected, indicating that inhibition of protein synthesis was caused by transcription inhibition by RBV. Using a recombinant green fluorescence protein-expressing hPIV-2 without matrix protein, it was found that RBV did not completely inhibit virus entry into the cells; however, it almost completely blocked multinucleated giant cell formation.

3.Cutaneous biodistribution of ionizable, biolabile aciclovir prodrugs after short duration topical iontophoresis: Targeted intraepidermal drug delivery.
Chen Y1, Zahui T1, Alberti I1, Kalia YN2. Eur J Pharm Biopharm. 2016 Feb;99:94-102. doi: 10.1016/j.ejpb.2015.11.010. Epub 2015 Nov 22.

The objective was to determine the cutaneous biodistribution of aciclovir (ACV), that is, the amount of drug as a function of depth within the skin following topical iontophoretic administration of amino acid ester prodrugs of ACV (ACV-X, where X=Arg, Ile or Val). The results were compared to those obtained with marketed formulations of aciclovir and penciclovir (PCV), and following topical iontophoresis of ACV. Quantification of molecules as a function of position in the skin was achieved by snap-freezing and cryotoming skin samples to obtain coarse or fine lamellae with a thickness of either 100μm or 20μm. The molecules - ACV, ACV-X or PCV - were extracted and quantified by validated UHPLC-MS/MS analytical methods. Passive delivery of ACV or PCV from marketed cream and ointment formulations after application for 60min resulted in modest cutaneous deposition (QDEP,ACV and QDEP,PCV<2nmol/cm(2)). Moreover, ACV and PCV were found mainly in the stratum corneum or superficial viable epidermis.

4.Indirect photochemical transformations of acyclovir and penciclovir in aquatic environments increase ecological risk.
An J1,2, Li G1, An T1, Nie X3. Environ Toxicol Chem. 2016 Mar;35(3):584-92. doi: 10.1002/etc.3238. Epub 2016 Feb 9.

Acyclovir and penciclovir, 2 antiviral drugs, are increasingly detected in aquatic environments. The present study explores the natural photochemical transformation mechanisms and fate of these drugs, examining direct and indirect photochemical transformation under simulated sunlight irradiation. The 2 antiviral drugs are photostable under certain conditions but significantly degrade in the presence of chromophoric dissolved organic matter (DOM). The degradation rate associated with the drugs' indirect photochemical transformation scaled with chromophoric DOM concentration. Quenchers and sensitizers were used to identify indirect photochemical transformation mechanism. Results suggested that both pharmaceuticals could be transformed by reacting with (1) O2 , (•) OH, and excited chromophoric DOM. The (1) O2 played an important role in indirect photochemical transformation. Furthermore, the reaction kinetics between their substructural molecules, guanine, isocytosine, and imidazole, with different reactive oxygen species were evaluated to determine which substrate functionalities were most susceptible to singlet oxygenation.

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