Vidarabine phosphate
(Synonyms: ara-AMP; ara-A 5'-monophosphate) 目录号 : GC67195Vidarabine phosphate (Ara-AMP) 是一种抗病毒剂,可抑制慢性乙型肝炎病毒 (HBV) 感染。Vidarabine phosphate 还可以对抗单纯疱疹病毒和水痘带状疱疹病毒。
Cas No.:29984-33-6
Sample solution is provided at 25 µL, 10mM.
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Vidarabine phosphate (Ara-AMP), an antiviral agent, inhibits chronic HBV infection[1][2]. Vidarabine phosphate also against herpes simplex and varicella zoster viruses[3].
[1]. A W Gough, et al. Comparison of the neonatal toxicity of two antiviral agents: vidarabine phosphate and cytarabine. Toxicol Appl Pharmacol. 1982 Oct;66(1):143-52.
[2]. C I Smith, et al. Vidarabine monophosphate and human leukocyte interferon in chronic hepatitis B infection. JAMA. 1982 Apr 23;247(16):2261-5.
[3]. D Kinchington. Recent advances in antiviral therapy. J Clin Pathol. 1999 Feb;52(2):89-94.
Cas No. | 29984-33-6 | SDF | Download SDF |
别名 | ara-AMP; ara-A 5'-monophosphate | ||
分子式 | C10H14N5O7P | 分子量 | 347.22 |
溶解度 | DMSO : 16.67 mg/mL (48.01 mM; ultrasonic and warming and heat to 60°C); H2O : 4.9 mg/mL (14.11 mM; ultrasonic and warming and adjust pH to 7 with NaOH and heat to 60°C) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.88 mL | 14.4001 mL | 28.8002 mL |
5 mM | 0.576 mL | 2.88 mL | 5.76 mL |
10 mM | 0.288 mL | 1.44 mL | 2.88 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
Formulation of a stable Vidarabine phosphate injection
Pharm Weekbl Sci 1984 Jun 22;6(3):101-4.PMID:6462876DOI:10.1007/BF01962998.
An injection fluid with Vidarabine phosphate (37.5 mg/ml, pH 7.4) was formulated. After steam sterilization for 20 min at 120 degrees C a 6.1% degradation was observed. No significant (p greater than 0.05) degradation could be observed after heating in steam for 30 min at 100 degrees C and after storage for four months at 4 degrees C. From the results of an investigation of the degradation rate at elevated temperatures a negligible loss of content after a three years' storage period at 4 degrees C could be predicted.
Recent advances in antiviral therapy
Clin Pharm 1986 Dec;5(12):961-76.PMID:3542344doi
Virus replication is described, and the clinical trials and indications for amantadine, rimantadine, vidarabine, Vidarabine phosphate, acyclovir, ribavirin, and other promising antiviral agents are reviewed. Amantadine and rimantadine are useful for the treatment and prophylaxis of viral influenza A infections. Vidarabine is a second-line agent and is effective for the treatment of herpes simplex encephalitis, neonatal herpes simplex types 1 and 2, and varicella-zoster infections. Vidarabine phosphate (also known as vidarabine monophosphate) has a similar spectrum of activity and can be administered in smaller volumes than vidarabine. Acyclovir has demonstrated clinical efficacy for chickenpox, shingles (herpes zoster), genital herpes, and other herpes simplex infections. Acyclovir is also useful for the suppression of herpes infections. Systemically administered ribavirin is indicated for the treatment of Lassa fever. Aerosol ribavirin is effective for the treatment of respiratory syncytial virus pneumonia in children and infants and influenza A infections in adults. Only acyclovir, amantadine, ribavirin, and vidarabine are used in clinical practice. Vidarabine phosphate and investigational agents such as rimantadine, ganciclovir (DHPG, BW B759U), phosphonoformate, and bromovinyl-deoxyuridine (BVDU) need further investigation.
Adenine arabinoside monophosphate (Vidarabine phosphate) in combination with human leukocyte interferon in the treatment of chronic hepatitis B. A randomized, double-blinded, placebo-controlled trial
Ann Intern Med 1987 Sep;107(3):278-85.PMID:2441633DOI:10.7326/0003-4819-107-2-278.
Study objective: To determine the efficacy of adenine arabinoside monophosphate (Ara-AMP Vidarabine phosphate) with or without human leukocyte interferon in chronic hepatitis B. Study design: Randomized, double-blinded, placebo-controlled trial with 6-month treatment and an 18-month follow-up. Setting: Referral-based liver-disease clinics at three university medical centers. Patients: Twenty-five patients with chronic active hepatitis or cirrhosis and 39 with chronic persistent hepatitis. Interventions: Thirteen patients received intramuscular Ara-AMP, 2.5 mg/kg body weight, twice daily, alternated monthly for 6 months with subcutaneous human leukocyte interferon, 5 million units, twice daily. Painful paresthesia of the legs necessitated dosage reduction and early discontinuation of enrollment. Twenty-four patients received intramuscular Ara-AMP, 2.5 mg/kg, twice daily, alternated monthly for 6 months with a matching placebo given subcutaneously twice daily. Twenty-seven patients received placebo by intramuscular and subcutaneous injections twice daily for 6 months. Measurements and main results: Of the 64 patients, 95% had symptomatic and virologic data available and 64% had biopsies at 12 months; at 24 months, 77% had data available and 56% had repeat biopsies. The highest dropout rate was seen in the group receiving Ara-AMP. The group receiving the placebo was less symptomatic (Karnofsky score of 96% compared with 91% in the group receiving Ara-AMP/placebo and 92% in the group receiving Ara-AMP/human leukocyte interferon, p = 0.02) at 12 but not at 24 months. Loss of DNA polymerase, the hepatitis B e antigen, and the serum hepatitis B virus DNA was similar in all three groups. Histologically, erosion of the limiting plate and lobular activity favored Ara-AMP at 12 but not at 24 months and these differences did not result in differences in the histologic diagnosis. Conclusion: These results do not support the use of Ara-AMP and human leukocyte interferon in chronic persistent or chronic active hepatitis B.