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69657-51-8价格

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69657-51-8

69657-51-8结构式
69657-51-8结构式
  • 常用中文名：阿昔洛韦钠
  • 常用英文名：Aciclovir sodium
  • CAS号：69657-51-8
  • 分子式：C8H10N5NaO3
  • 分子量：247.18600
  • 相关类别： 原料药 人工合成抗感染类药 抗病毒类药
  • 发布时间：2018-04-28 08:00:00
  • 更新时间：2024-01-02 16:58:40
  • 阿昔洛韦钠是一种有效的口服抗病毒药物。阿昔洛韦钠具有抗疱疹活性,对HSV-1和HSV-2的IC50值分别为0.85μM和0.86μM。阿昔洛韦钠诱导细胞周期紊乱和凋亡。阿昔洛韦钠预防急性白血病诱导治疗期间的细菌感染[1][2][3][4]。

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中文名 阿昔洛韦钠
英文名 Sodium 2-((2-amino-6-oxo-1H-purin-9(6H)-yl)methoxy)ethanolate
中文别名 9-(2-羟乙氧甲基)鸟嘌呤钠
注射用阿昔洛韦
英文别名 Aciclovir sodium
描述 阿昔洛韦钠是一种有效的口服抗病毒药物。阿昔洛韦钠具有抗疱疹活性,对HSV-1和HSV-2的IC50值分别为0.85μM和0.86μM。阿昔洛韦钠诱导细胞周期紊乱和凋亡。阿昔洛韦钠预防急性白血病诱导治疗期间的细菌感染[1][2][3][4]。
相关类别
靶点

HSV-1:0.85 μM (IC50)

HSV-2:0.86 μM (IC50)

体外研究 阿昔洛韦钠(3-100µM；24-72小时；Jurkat、U937和K562白血病细胞)以剂量和时间依赖性降低细胞存活率[1]。阿昔洛韦钠(10-100µM；24-72小时；Jurkat细胞)阻断DNA合成,从而阻止细胞周期进入G2/M和S期,并以剂量依赖性方式增加亚G1亚二倍体峰[1]。阿昔洛韦钠(10-100µM；24-72小时；Jurkat细胞)通过激活caspase-3和存在核DNA碎片诱导凋亡[1]。细胞存活率测定[1]细胞系：Jurkat、U937和K562白血病细胞浓度：3、10、30和100µM孵育时间：24、48和72小时结果：细胞存活率呈剂量和时间依赖性降低。凋亡分析[1]细胞系：Jurkat细胞浓度：10和100µM孵育时间：24、48和72小时结果：caspase-3活性增加并切割核间体DNA。细胞周期分析[1]细胞系：Jurkat细胞浓度：10和100µM孵育时间：24、48和72小时结果：24和48小时后,细胞在S期呈剂量依赖性聚集。72小时后,亚G1亚二倍体峰呈剂量依赖增加。
体内研究 阿昔洛韦钠(20 mg/kg；p.o.；每日三次；持续10天；BALB/c小鼠)抑制皮肤损伤的发展,并导致DTH反应和抗体产生之间的分离[3]动物模型：感染HSV-1的特异性无病原体BALB/c小鼠(7周龄)[3]剂量：20 mg/千克给药：口服给药；每日三次；10天结果：抑制皮肤损伤的发展,导致DTH反应和抗体产生之间的分离。
参考文献

[1]. 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.

[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]. 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.

[4]. 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.
沸点 613.1ºC at 760 mmHg
分子式 C8H10N5NaO3
分子量 247.18600
精确质量 247.06800
PSA 122.14000
LogP 0.09990
储存条件 库房通风低温干燥,与食品原料分开存放

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UP0791500
CHEMICAL NAME :
6H-Purin-6-one, 1,9-dihydro-2-amino-9-((2-hydroxyethoxy)methyl)-, monosodium salt
CAS REGISTRY NUMBER :
69657-51-8
LAST UPDATED :
199612
DATA ITEMS CITED :
15
MOLECULAR FORMULA :
C8-H10-N5-O3.Na
MOLECULAR WEIGHT :
247.22

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
107 mg/kg/5D-I
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - hallucinations, distorted perceptions Behavioral - toxic psychosis
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - child
DOSE/DURATION :
248 mg/kg/80H-I
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>20 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1210 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
650 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>600 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>10 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
999 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
405 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - ataxia
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
1550 mg/kg/31D-I
TOXIC EFFECTS :
Gastrointestinal - other changes Kidney, Ureter, Bladder - urine volume decreased Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
300 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
300 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
300 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - delayed effects
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
100 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - endocrine system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

MUTATION DATA

TEST SYSTEM :
Rodent - mouse
DOSE/DURATION :
1995 umol/kg/24H (Intermittent)
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 369,65,1996

危害码 (欧洲) C
海关编码 2933990090
海关编码 2933990090
中文概述 2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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