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Abacavir

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纯度: 99.81%

货号 T1267Cas号 136470-78-5

别名 阿巴卡韦, Ziagen, Epzicom

Abacavir (Ziagen) 是一种核苷类似物逆转录酶抑制剂。

Abacavir
其他形式的 “Abacavir”:

Abacavir

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Rating icon 很棒

纯度: 99.81%

货号 T1267 别名 阿巴卡韦, Ziagen, EpzicomCas号 136470-78-5

Abacavir (Ziagen) 是一种核苷类似物逆转录酶抑制剂。

规格价格库存数量
5 mg
¥ 279
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10 mg
¥ 393
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25 mg
¥ 659
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50 mg
¥ 898
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100 mg
¥ 1,130
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200 mg
¥ 1,430
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500 mg
¥ 2,430
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1 g
¥ 3,620
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1 mL x 10 mM (in DMSO)
¥ 323
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产品介绍


Abacavir AI Summary
Abacavir exhibits broad antiviral activity and cytostatic properties across various viral strains and cell lines. It demonstrates significant efficacy against HIV-1 Reverse Transcriptase, including both wild type and M184V mutant with EC50 values of 5300.0 nM and 15500.0 nM, respectively. Its activity against HIV-1 replication in CEM cells is notable, with an EC50 of 1600.0 nM and a cytotoxicity CC50 of 83000.0 nM. Furthermore, it shows antiviral activity against HIV-2 with EC50 values ranging from 3000.0 nM to 7300.0 nM, and herpes simplex virus types 1 and 2. In HBV mutants, Abacavir achieves 80.0% and 72.0% inhibition against M204I and L180M/M204V mutants, respectively, with an overall EC50 of 3400.0 nM. Additionally, it is potent against multidrug-resistant HIV-1 strains, demonstrated by fold change values ranging from 1.4 to 29.0 relative to wild type. The compound also shows high oral bioavailability at 86.0% in humans, suggesting effective systemic uptake when administered orally. Abacavir displays inhibitory effects on different enzymes and receptors, including Histone Lysine Methyltransferase G9a, and exhibits liver toxicity as indicated by a high DILI severity score of 8.0. It shows relatively low clearance rates and short half-life in humans. The compound's pharmacokinetic profile reveals gender-specific differences in drug metabolism. Despite its antiviral properties, Abacavir has a moderate bioactivity profile, with some cytotoxicity against various human cell lines and a non-significant inhibition of P-gp. It has limited binding affinity for human serum albumin and shows potential hepatotoxicity based on liver function tests. Additionally, Abacavir has an IC50 value greater than 20000.0 nM for SARS-CoV-2, indicating low potency in this context. Overall, these characteristics underscore its potential for further development in antiviral therapies, albeit with considerations for associated hepatotoxic risks..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Abacavir (Ziagen) is a nucleoside reverse transcriptase inhibitor analog of guanosine. This agent decreases HIV viral loads, retards or prevents the damage to the immune system, and reduces the risk of developing AIDS.
别名阿巴卡韦, Ziagen, Epzicom
化学信息
分子量286.33
分子式C14H18N6O
CAS No.136470-78-5
SmilesN(C1=C2C(N(C=N2)[C@@H]3C[C@H](CO)C=C3)=NC(N)=N1)C4CC4
密度1.70 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 250 mg/mL (873.12 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.98 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.4925 mL17.4624 mL34.9247 mL174.6237 mL
5 mM0.6985 mL3.4925 mL6.9849 mL34.9247 mL
10 mM0.3492 mL1.7462 mL3.4925 mL17.4624 mL
20 mM0.1746 mL0.8731 mL1.7462 mL8.7312 mL
50 mM0.0698 mL0.3492 mL0.6985 mL3.4925 mL
100 mM0.0349 mL0.1746 mL0.3492 mL1.7462 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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