Acyclovir-d4
(Synonyms: 阿昔洛韦D4,Aciclovir-d4; Acycloguanosine-d4) 目录号 : GC46797
An internal standard for the quantification of acyclovir
Cas No.:1185179-33-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Acyclovir-d4 is intended for use as an internal standard for the quantification of acyclovir by GC- or LC-MS. Acyclovir is a guanosine analog that has antiviral activity in vitro against the herpes simplex viruses, varicella zoster virus, Epstein-Barr virus, cytomegalovirus, and human herpes virus 6 (ID50s = 0.1-63.1 μM).1 It diffuses freely into cells and is selectively converted into acyclo-guanosine monophosphate by a virus-specific thymidine kinase. During DNA replication, the phosphorylated form of acyclovir is preferentially incorporated into viral DNA, resulting in premature chain termination and inhibition of further DNA polymerase activity.2 Acyclovir (5 mg/kg) reduces viral titers in mice infected with the herpes simplex virus-1 (HSV-1) strain SC16.3
1.Balfour, H.H., Jr.Management of cytomegalovirus disease with antiviral drugsRev.Infect.Dis.12(Suppl. 7)S849-S860(1990) 2.Bean, B.Antiviral therapy: Current concepts and practicesClin.Microbiol.Rev.5(2)146-182(1992) 3.Ashton, R.J., Abbott, K.H., Smith, G.M., et al.Antiviral activity of famciclovir and acyclovir in mice infected intraperitoneally with herpes simplex virus type 1 SC16J. Antimicrob. Chemother.34(2)287-290(1994)
| Cas No. | 1185179-33-2 | SDF | |
| 别名 | 阿昔洛韦D4,Aciclovir-d4; Acycloguanosine-d4 | ||
| Canonical SMILES | O=C1C2=C(N(COC([2H])([2H])C([2H])([2H])O)C=N2)N=C(N)N1 | ||
| 分子式 | C8H7D4N5O3 | 分子量 | 229.2 |
| 溶解度 | DMSO: Soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.363 mL | 21.815 mL | 43.63 mL |
| 5 mM | 0.8726 mL | 4.363 mL | 8.726 mL |
| 10 mM | 0.4363 mL | 2.1815 mL | 4.363 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Controlled ex-vivo plasma hydrolysis of valaciclovir to acyclovir demonstration using tandem mass spectrometry
Biomed Chromatogr 2011 Nov;25(11):1189-200.PMID:21400550DOI:10.1002/bmc.1590
Plasma estimation of valaciclovir, an antiviral drug, is challenging due to both in-vivo and ex-vivo hydrolysis to active metabolite acyclovir. A simultaneous method is described involving the solid-phase ion-exchange extraction procedure requiring 100 μL of plasma volume, a reverse-phase Lichrosphere RP Select B (125 × 6 mm, 5 μm) column and isocratic mobile phase to achieve the desired chromatographic separation. ESI-MS/MS multiple reaction monitoring in positive polarity, detected mass pairs for valaciclovir (m/z 325.5 → 152.2), acyclovir (m/z 226.3 → 152.2) and respective internal standards valganciclovir (m/z 307.1 → 220.3) and Acyclovir-d4 (m/z 230.2 → 152.0). Fully fledged method validation was evaluated as per current regulatory requirements and results were deemed acceptable. The plasma samples showed extensive hydrolysis of valaciclovir when collected or processed at room temperature, without buffer stabilization prior to storage at -15°C. Our results showed that using prechilled K3 EDTA vacutainers immersed in an iced-water bath during blood sample collection, and addition of 50% orthophosphoric acid solution to plasma samples prior to storage at -50°C for at least 120 days controlled the hydrolysis of valaciclovir to acyclovir. While monitoring drug absorption into systematic circulation, the valaciclovir to acyclovir formation ratio was improved to 1:20 in healthy volunteers for the first time.