产品说明书

Penciclovir

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Chemical Structure| 39809-25-1 同义名 : BRL 39123;VSA 671
CAS号 : 39809-25-1
货号 : A135007
分子式 : C10H15N5O3
纯度 : 98%
分子量 : 253.26
MDL号 : MFCD00866931
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(98.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2 mg/mL(7.9 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 Penciclovir is a synthetic acyclic guanine derivative with antiviral activity, mainly used to treat infections from herpes simplex virus (HSV) types 1 and 2. In HSV infected cells, penciclovir is phosphorylated by viral thymidine kinase and subsequently converted by cellular kinases into the active metabolite, penciclovir triphosphate, which competitively inhibits viral HSV polymerase by blocking deoxyguanosine triphosphate substrate binding[3]. Penciclovir are phosphorylated by viral thymidine kinase and are incorporated into the DNA chain by viral DNA polymerase, resulting in chain termination[4]. Penciclovir pharmacokinetics following oral administration of famciclovir were nonlinear within the dosage range studied, likely because of saturation of famciclovir metabolism. Oral administration of famciclovir at 40 or 90 mg/kg produced similar C(max) and time to C(max) values. Therefore, the lower dose may have similar antiviral efficacy to that proven for the higher dose[5]. Oral administration of 40 mg of famciclovir/kg to cats resulted in a tear penciclovir concentration-time profile that approximated the plasma penciclovir concentration-time profile and frequently achieved a penciclovir concentration at the ocular surface likely to be effective against FHV-1(feline herpesvirus) [6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01832974 Adrenocortical Carcinoma Phase 1 Terminated(Business decision b... 展开 >>y the sponsor during Phase 1.) 收起 << - United States, Maryland ... 展开 >> National Cancer Institute at the National Institutes of Health Bethesda, Maryland, United States, 20892 收起 <<
NCT02696811 DNA Damage In... 展开 >>flammation 收起 << Not Applicable Completed - United Kingdom ... 展开 >> Agriculture Building, Newcastle University Newcastle upon Tyne, Tyne and Wear, United Kingdom, NE1 7RU 收起 <<
NCT02423668 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.95mL

0.79mL

0.39mL

19.74mL

3.95mL

1.97mL

39.49mL

7.90mL

3.95mL
参考文献

[1]Amjad M, Gillespie MA, et al. Flow cytometric evaluation of antiviral agents against human herpesvirus 6. Microbiol Immunol. 2001;45(3):233-40.

[2]Earnshaw DL, Bacon TH, et al. Mode of antiviral action of penciclovir in MRC-5 cells infected with herpes simplex virus type 1 (HSV-1), HSV-2, and varicella-zoster virus. Antimicrob Agents Chemother. 1992 Dec;36(12):2747-57.

[3]Mohammed AF, Andrei G, Hayallah AM, Abdel-Moty SG, Snoeck R, Simons C. Synthesis and anti-HSV activity of tricyclic penciclovir and hydroxybutylguanine derivatives. Bioorg Med Chem. 2019 Mar 15;27(6):1023-1033

[4]Shiraki K. Antiviral Drugs Against Alphaherpesvirus. Adv Exp Med Biol. 2018;1045:103-122

[5]Thomasy SM, Whittem T, Bales JL, Ferrone M, Stanley SD, Maggs DJ. Pharmacokinetics of penciclovir in healthy cats following oral administration of famciclovir or intravenous infusion of penciclovir. Am J Vet Res. 2012 Jul;73(7):1092-9

[6]Thomasy SM, Covert JC, Stanley SD, Maggs DJ. Pharmacokinetics of famciclovir and penciclovir in tears following oral administration of famciclovir to cats: a pilot study. Vet Ophthalmol. 2012 Sep;15(5):299-306