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Tizanidine
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很棒纯度: 99.11%
货号 T7065Cas号 51322-75-9
别名 替扎尼定
Tizanidine 是一种 α2-肾上腺素受体激动剂，能够抑制神经递质从CNS 去甲肾上腺素激活的神经元中释放。
其他形式的 “Tizanidine”:
Tizanidine
一键复制产品信息 很棒纯度: 99.11%
货号 T7065 别名 替扎尼定Cas号 51322-75-9
Tizanidine 是一种 α2-肾上腺素受体激动剂，能够抑制神经递质从CNS 去甲肾上腺素激活的神经元中释放。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 2 mg | ¥ 119 | 现货 | |
| 5 mg | ¥ 179 | 现货 | |
| 10 mg | ¥ 288 | 现货 | |
| 25 mg | ¥ 462 | 现货 | |
| 50 mg | ¥ 668 | 现货 | |
| 100 mg | ¥ 892 | 现货 | |
| 500 mg | ¥ 2,270 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 198 | 现货 |
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产品介绍
Tizanidine AI Summary
Tizanidine is a biologically active compound with diverse pharmacokinetic and pharmacodynamic properties. It has a partition coefficient (LogD6.5) of -0.68 and a delta logD of -0.81 between pH 6.5 and 7.4. The compound’s ionization constant (pKa) is 8.0, reflecting its ionization behavior. It demonstrates moderate oral bioavailability in humans at 49%, alongside high solubility at pH 7.4 (600 μM) and pH 7.2 (18,250 μg/mL).
In terms of distribution and clearance, Tizanidine has a volume of distribution at steady state (Vdss) of 2.4 L/kg and high binding to plasma proteins with a fraction unbound (Fu) of 0.7. It shows a total body clearance of 11.0 mL/min/kg and a renal clearance of 0.33 mL/min/kg, indicating significant renal excretion and suggesting efficient clearance from the body. The hepatic clearance is low at 10.7 mL/min/kg.
Tizanidine displays bioactivity at several targets. It displaces [125I]PIC from human alpha2 adrenoceptors and human imidazoline receptor 1, with Ki values of 117.9 nM and 28.31 nM respectively, and a selectivity ratio of 0.6197 favoring imidazoline receptor 1. It also inhibits human FAAH at 1 μM concentration, demonstrating 7.43% inhibition. Additionally, it inhibits a range of enzymes and receptors, including moderate inhibition of SARS-CoV-2 3CL-Pro protease and binding activities towards various adrenergic and histamine receptors.
Pharmacodynamically, Tizanidine shows efficacy as an agonist at alpha-2A and alpha-2C adrenergic receptors, inhibiting forskolin-stimulated cAMP accumulation with an EC50 of 86.0 nM for alpha-2A. It presents antiviral activity against SARS-CoV-2 and demonstrated moderate inhibition of induced cytotoxicity in VERO-6 cells at a concentration of 10 μM.
However, Tizanidine is also associated with significant hepatotoxic effects, as evidenced by elevated liver enzymes such as ALT, AST, and others. It can induce conditions like cholelithiasis, cirrhosis, hepatic failure, and hepatitis, suggesting a need for caution in its therapeutic use.
Overall, Tizanidine represents a multi-faceted pharmaceutical agent with notable pharmacological actions and potential bioactivities against various biological targets, but caution is warranted due to its association with liver toxicity..
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 | Tizanidine, an α2-adrenergic receptor agonist, suppresses the release of neurotransmitters from central nervous system (CNS) noradrenergic neurons. |
| 别名 | 替扎尼定 |
| 分子量 | 253.71 |
| 分子式 | C9H8ClN5S |
| CAS No. | 51322-75-9 |
| Smiles | N(C=1C=2C(C=CC1Cl)=NSN2)C=3NCCN3 |
| 密度 | 1.82 g/cm3 |
| 存储 | keep away from direct sunlight,store at low temperature | 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: 4.4 mg/mL (17.34 mM), Sonication is recommended.  | ||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.94 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
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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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