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Didanosine
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很棒纯度: 99.64%
货号 T2578Cas号 69655-05-6
别名 去羟肌苷, 地丹诺辛, ddI, 2',3'-Dideoxyinosine
Didanosine (ddI) 是一种逆转录酶抑制剂，IC50为490nM。
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Didanosine
一键复制产品信息 很棒纯度: 99.64%
货号 T2578 别名 去羟肌苷, 地丹诺辛, ddI, 2',3'-DideoxyinosineCas号 69655-05-6
Didanosine (ddI) 是一种逆转录酶抑制剂，IC50为490nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 140 | 现货 | |
| 10 mg | ¥ 252 | 现货 | |
| 25 mg | ¥ 367 | 现货 | |
| 50 mg | ¥ 476 | 现货 | |
| 100 mg | ¥ 678 | 现货 | |
| 500 mg | ¥ 1,710 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 273 | 现货 |
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产品介绍
Didanosine AI Summary
Didanosine exhibits a range of pharmacological and biological activities, particularly in the context of antiviral efficacy against HIV-1 and HIV-2. It shows potent antiviral activity with EC50 values varying between 2,710 nM and 23,200 nM in various assays conducted on human MT4, CEM, and PBMC cell lines. The compound demonstrates selectivity indices, calculated as the ratio of CC50 (cytotoxicity) to EC50 (antiviral activity), which indicate a favorable therapeutic profile. For instance, the selectivity index for HIV-1 3B infected MT4 cells is greater than 9.0, suggesting a good balance between efficacy and safety.
In addition to HIV, Didanosine exhibits antiviral activity against HSV-1 with significant EC50 values. It also indicates potential cytotoxicity in various cell lines, with CC50 values generally exceeding 100,000 nM, demonstrating a high threshold for cytotoxic effects compared to its antiviral activity. Furthermore, the compound has a logP of -1.24, suggesting specific solubility characteristics that may influence its bioavailability and distribution.
The compound also shows antiviral activities against other viruses, including Hepatitis B virus, with an EC50 > 10,000 nM in the 2.2.15 cell line, and limited activity against SARS-CoV-2.
Pharmacokinetic data reveal moderate clearance rates, a volume of distribution at steady state (Vdss) of 0.77 L·kg-1, a high fraction unbound (Fu) of 0.95, and a short half-life in humans. The compound displays hepatotoxic potential as indicated by the FDA Liver Toxicity Knowledge Base and various clinical-chemistry assays, despite a favorable therapeutic index in antiviral applications.
The compound has also shown low to moderate activity in various cellular assays involving enzymes and protein-protein interactions, with most IC50 values being relatively high, indicating limited potency against those targets. Overall, Didanosine represents a promising antiviral agent, particularly for HIV, with a high selectivity for viral eradication over cytotoxic effects, though caution is warranted due to potential hepatotoxicity..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Didanosine (ddI) is a nucleoside reverse transcriptase inhibitor analog of adenosine (IC50: 0.49 μM). |
| 靶点活性 | Reverse transcriptase:0.49 μM |
| 体内活性 | 在培养的人类肌肉细胞中,Didanosine可促使胞浆脂滴积累,增加乳酸生产,减少SDH（复合物II的一部分）和COX（复杂IV）的活性。在HIV靶细胞中,Didanosine转化为它的活性形式脱氧腺苷-5'-三磷酸（ddATP）。在解离的DRG细胞培养中,Didanosine剂量依赖性地诱导神经突数目、最长神经突中的每个神经元长度及神经突的总长度的减少。在解离的DRG神经元中,Didanosine剂量依赖性地诱导神经突回缩或轴突损失,说明去羟肌苷对发展周围神经病变有一定帮助。在培养的人TK6淋巴母细胞中,Didanosine对齐多呋定引起的胸苷激酶基因的致突变性有诱导作用。 |
| 别名 | 去羟肌苷, 地丹诺辛, ddI, 2',3'-Dideoxyinosine |
| 分子量 | 236.23 |
| 分子式 | C10H12N4O3 |
| CAS No. | 69655-05-6 |
| Smiles | O=C1C2=C(N(C=N2)[C@@H]3O[C@H](CO)CC3)NC=N1 |
| 密度 | 1.2917 g/cm3 (Estimated) |
| 存储 | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 70 mg/mL (296.32 mM), Sonication is recommended.  H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (8.47 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 | ||||||||||||||||||||||||||||||||||||
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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：
比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL， 一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O， 那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 100 μL DMSO （ 母液浓度为 20 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： 取 100 μL DMSO 母液， 添加 400 μL PEG300 混匀澄清， 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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。
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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