标签归档：aciclovir

Acyclovir-d4(Synonyms: Aciclovir-d4; Acycloguanosine-d4)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Acyclovir-d4 (Synonyms: Aciclovir-d4; Acycloguanosine-d4)

Acyclovir-d4 (Aciclovir-d4) 是 Acyclovir 的氘代物。Acyclovir (Aciclovir) 是一种鸟嘌呤类似物和一种具有口服活性的抗病毒剂。Acyclovir 具有抗 HSV-1 (IC50 为 0.85 μM)，HSV-2 (IC50 为 0.86 μM) 和水痘带状疱疹病毒的活性。Acyclovir 可被病毒胸苷激酶 (TK) 磷酸化，Acyclovir triphosphate 可干扰病毒 DNA 聚合。Acyclovir 可预防急性白血病的诱导疗法中的细菌感染。

Acyclovir-d4(Synonyms: Aciclovir-d4; Acycloguanosine-d4)

Acyclovir-d4 Chemical Structure

CAS No. : 1185179-33-2

规格 价格 是否有货
1 mg ￥3500 询问价格 & 货期
5 mg ￥14000 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Acyclovir-d4 (Aciclovir-d4) is the deuterium labeled Acyclovir. Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

229.23

Formula

C8H7D4N5O3
CAS 号

1185179-33-2
中文名称

阿昔洛韦 d4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Li Z, et al. Acyclovir treatment of skin lesions results in immune deviation in mice infected cutaneously with herpes simplex virus. Antivir Chem Chemother. 1999 Sep;10(5):251-7.

    [3]. Suzuki M, et al. Synergistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61.

    [4]. Benedetti S, et al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity. Life Sci. 2018 Dec 15;215:80-85.

    [5]. Hayashi K, et al. The role of a HSV thymidine kinase stimulating substance, scopadulciol, in improving the efficacy of cancer gene therapy. J Gene Med. 2006 Aug;8(8):1056-67.

    [6]. Lönnqvist B, et al. Oral acyclovir as prophylaxis for bacterial infections during induction therapy for acute leukaemia in adults. The Leukemia Group of Middle Sweden. Support Care Cancer. 1993 May;1(3):139-44.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Acyclovir(Synonyms: 阿昔洛韦; Aciclovir; Acycloguanosine)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Acyclovir (Synonyms: 阿昔洛韦; Aciclovir; Acycloguanosine) 纯度: 99.34%

Acyclovir (Aciclovir) 是一种鸟嘌呤类似物和一种具有口服活性的抗病毒剂。Acyclovir 具有抗 HSV-1 (IC50 为 0.85 μM)，HSV-2 (IC50 为 0.86 μM) 和水痘带状疱疹病毒的活性。Acyclovir 可被病毒胸苷激酶 (TK) 磷酸化，Acyclovir triphosphate 可干扰病毒 DNA 聚合。Acyclovir 可预防急性白血病的诱导疗法中的细菌感染。

Acyclovir(Synonyms: 阿昔洛韦; Aciclovir; Acycloguanosine)

Acyclovir Chemical Structure

CAS No. : 59277-89-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605 In-stock
50 mg ￥550 In-stock
100 mg ￥880 In-stock
500 mg ￥1500 In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

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生物活性

Acyclovir (Aciclovir) is a guanosine analogue and an orally active antiviral agent. Acyclovir inhibits HSV-1 (IC50 of 0.85 μM), HSV-2 (IC50 of 0.86 μM) and varicella-zoster virus. Acyclovir can be phosphorylated by viral thymidine kinase (TK), and Acyclovir triphosphate interferes with viral DNA polymerization through competitive inhibition with guanosine triphosphate and obligatory chain termination[1][2][3]. Acyclovir prevents bacterial infections during induction therapy for acute leukaemia[4].

IC50 & Target[1][2]

HSV-1

0.85 μM (IC50)

HSV-2

0.86 μM (IC50)

Bacterial

 

体外研究
(In Vitro)

Acyclovir (3-100 µM; 24-72 hours; Jurkat, U937, and K562 leukemia cells) treatment shows a dose- and time-dependent reduction of cell viability[3].
Acyclovir (10-100 µM; 24-72 hours; Jurkat cells) treatment shows a delay/block in S phase and an increase of the sub-G1 peak[3].
Acyclovir (10-100 µM; 24-72 hours; Jurkat cells) treatment activates caspase-3 and presences nuclear DNA fragmentation, thereby indicating apoptotic cell death[3].
In HSV-infected cells, HSV thymidine kinase (HSV-TK) specifically phosphorylate Acyclovir to its monophosphate, and this activation confers a high degree of selectivity of the drugs. Thereafter, the monophosphate is further phosphorylated to the diphosphate (Acyclovir -DP) and triphosphate (Acyclovir -TP) by cellular kinases. The triphosphate is the fully activated metabolite that is toxic to the virus[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[3]

Cell Line: Jurkat, U937, and K562 leukemia cells
Concentration: 3 µM, 10 µM, 30 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Showed a dose- and time-dependent reduction of cell viability.

Cell Cycle Analysis[3]

Cell Line: Jurkat cells
Concentration: 10 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Revealed a dose-dependent accumulation of cells in S phase after 24 and 48 h. Showed a dose-dependent increase of the sub-G1 hypodiploid peak after 72 h.

Apoptosis Analysis[3]

Cell Line: Jurkat cells
Concentration: 10 µM, 100 µM
Incubation Time: 24 hours, 48 hours, and 72 hours
Result: Induced cell apoptosis.

体内研究
(In Vivo)

Acyclovir (20 mg/kg; oral administration; three times daily; for 10 days; BALB/c mice) treatment in infected mice suppresses the development of skin lesions and results in a dissociation between DTH response and antibody production[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Specific-pathogen-free BALB/c mice (7-week-old) infected with HSV-1[1]
Dosage: 20 mg/kg
Administration: Oral administration; three times daily; for 10 days
Result: Suppressed the development of skin lesions and resulted in a dissociation between DTH response and antibody production.

Clinical Trial

分子量

225.20

Formula

C8H11N5O3
CAS 号

59277-89-3
中文名称

阿昔洛韦；阿昔洛维；开糖环鸟苷；羟乙氧甲鸟嘌呤；无环鸟嘌呤核苷；无环鸟嘌呤；无环鸟苷
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (222.02 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4405 mL 22.2025 mL 44.4050 mL
5 mM 0.8881 mL 4.4405 mL 8.8810 mL
10 mM 0.4440 mL 2.2202 mL 4.4405 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.10 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.10 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Li Z, et al. Acyclovir treatment of skin lesions results in immune deviation in mice infected cutaneously with herpes simplex virus. Antivir Chem Chemother. 1999 Sep;10(5):251-7.

    [2]. Suzuki M, et al. Synergistic antiviral activity of acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus. Antiviral Res. 2006 Nov;72(2):157-61.

    [3]. Benedetti S, et al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity. Life Sci. 2018 Dec 15;215:80-85.

    [4]. Hayashi K, et al. The role of a HSV thymidine kinase stimulating substance, scopadulciol, in improving the efficacy of cancer gene therapy. J Gene Med. 2006 Aug;8(8):1056-67.

    [5]. Lönnqvist B, et al. Oral acyclovir as prophylaxis for bacterial infections during induction therapy for acute leukaemia in adults. The Leukemia Group of Middle Sweden. Support Care Cancer. 1993 May;1(3):139-44.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务