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Terfenadine
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很棒纯度: 99.75%
货号 T1266Cas号 50679-08-8
别名 特非那定, MDL-991, (±)-Terfenadine
Terfenadine ((±)-Terfenadine) 是一种hERG 开放通道抑制剂，IC50为 204 nM。它也是一种 H1 组胺受体拮抗剂，通过调节Ca2+稳态在黑素瘤细胞中起到有效的细胞凋亡诱导作用。 Terfenadine 诱导 ROS 依赖性细胞凋亡，同时激活Caspase-4，-2，-9。
其他形式的 “Terfenadine”:
Terfenadine
一键复制产品信息 很棒纯度: 99.75%
货号 T1266 别名 特非那定, MDL-991, (±)-TerfenadineCas号 50679-08-8
Terfenadine ((±)-Terfenadine) 是一种hERG 开放通道抑制剂，IC50为 204 nM。它也是一种 H1 组胺受体拮抗剂，通过调节Ca2+稳态在黑素瘤细胞中起到有效的细胞凋亡诱导作用。 Terfenadine 诱导 ROS 依赖性细胞凋亡，同时激活Caspase-4，-2，-9。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 50 mg | ¥ 236 | 现货 | |
| 100 mg | ¥ 413 | 现货 | |
| 200 mg | ¥ 588 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 148 | 现货 |
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产品介绍
Terfenadine AI Summary
Terfenadine exhibits diverse bioactivities across various biological assays, revealing a multifaceted pharmacological profile. Notably, it demonstrates potent inhibition of the K+ channel HERG, with IC50 values ranging from 56.0 nM to 213.8 nM, indicating significant cardiotoxic potential. Additionally, it shows strong antagonism of the human histamine H1 receptor with IC50 values of 94.0 nM and a dissociation constant (Kd) between 31.62 nM and 33.0 nM. In the field of immunology, it inhibits IL-4 and IL-5 production in mice splenocytes with IC50 values of 4950.0 nM and 3960.0 nM, respectively. The compound also exhibits moderate inhibition of cytochrome P450 enzymes, including CYP3A4 and CYP2J2, suggesting potential drug-drug interactions. In terms of pharmacokinetics, Terfenadine possesses a lengthy half-life of 23.0 hours in humans, a high plasma protein binding rate of 98.0%, and a volume of distribution of 2.9 L/kg. Additionally, the compound displays lipophilicity with a LogP value of 5.7 and shows inhibitory activity against various transporters, including P-glycoprotein. Furthermore, it demonstrates moderate antimicrobial activity against multiple strains of Plasmodium falciparum and Staphylococcus aureus. Overall, Terfenadine’s extensive bioactivity spectrum across multiple biological targets and its pharmacokinetic characteristics make it an intriguing subject for further research in various therapeutic areas..
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 | Terfenadine ((±)-Terfenadine) is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistaminic and non-sedative effects. |
| 靶点活性 | ERG (human):204 nM |
| 别名 | 特非那定, MDL-991, (±)-Terfenadine |
| 分子量 | 471.67 |
| 分子式 | C32H41NO2 |
| CAS No. | 50679-08-8 |
| Smiles | CC(C)(C)c1ccc(cc1)C(O)CCCN1CCC(CC1)C(O)(c1ccccc1)c1ccccc1 |
| 密度 | 1.0488 g/cm3 (Estimated) |
| 存储 | keep away from moisture | 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: 47.2 mg/mL (100.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.24 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20g，给药体积100 μL， 一共给药动物10只，您使用的配方为5%
DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O， 那么您的工作液浓度为2mg/mL。 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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