Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rizatriptan benzoate (MK-462 Benzoate) 是 5-HT1激动剂,通过选择性结合并激活血清素 (5-HT) 1B 受体和 5-HT 1D 受体,从而缓解偏头痛。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 178 | 现货 | ||
10 mg | ¥ 345 | 现货 | ||
25 mg | ¥ 712 | 现货 | ||
50 mg | ¥ 1,290 | 现货 | ||
100 mg | ¥ 1,950 | 现货 | ||
200 mg | ¥ 2,880 | 现货 | ||
500 mg | ¥ 4,720 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 357 | 现货 |
产品描述 | Rizatriptan benzoate (MK-462 Benzoate) selectively binds to and activates serotonin (5-HT) 1B receptors and 5-HT 1D receptors providing relief of migraine headaches. |
体内活性 | Rizatriptan blocks neurogenic vasodilation via an action on 5-HT(1D) receptors located on perivascular trigeminal nerves to inhibit CGRP release in anaesthetized guinea-pigs. Rizatriptan evokes a transient reduction in dural blood vessel diameter which recovered to baseline values within 10?min in anaesthetized guinea-pigs. [1] Rizatriptan significantly inhibits dural plasma protein extravasation produced by high intensity electrical stimulation of the trigeminal ganglion. Rizatriptan significantly reduces electrically stimulated dural vasodilation in anaesthetised rats. [2] Rizatriptan Benzoate significantly reduced SP mRNA levels in the midbrains of normal and model group rats, indicating that Rizatriptan Benzoate can downregulate SP gene expression in the rat midbrain. Rizatriptan Benzoate significantly reduces midbrain PENK mRNA expression, decreasing the levels of midbrain met-enkephalin and leu-enkephalin, and thereby weakening the analgesic effects of the endogenous pain modulatory system in rat model of migraine. [3] Rizatriptan Benzoate leads to the number of Fos-like immunoreactive neurons decreased in the spinal trigeminal nucleus caudal partand raphe magnus nucleus, increased the number of Fos-like immunoreactive neurons in the periaqueductal gray and remained unchanged in the ventromedial hypothalamic nucleus and mediodorsal thalamus nucleus in conscious rats. [4] Rizatriptan Benzoate markedly reduces the number of head-flicks in the rats. Rizatriptan Benzoate also significantly reduces the duration of grooming behavior by nearly 2-fold when compared with that without treatment. [5] |
别名 | 苯甲酸利扎曲坦, MK-462 Benzoate |
分子量 | 391.47 |
分子式 | C22H25N5O2 |
CAS No. | 145202-66-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16.67 mg/mL (42.57 mM), Sonication is recommended.
H2O: 39.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.5545 mL | 12.7724 mL | 25.5447 mL | 63.8619 mL |
5 mM | 0.5109 mL | 2.5545 mL | 5.1089 mL | 12.7724 mL | |
10 mM | 0.2554 mL | 1.2772 mL | 2.5545 mL | 6.3862 mL | |
20 mM | 0.1277 mL | 0.6386 mL | 1.2772 mL | 3.1931 mL | |
H2O | 50 mM | 0.0511 mL | 0.2554 mL | 0.5109 mL | 1.2772 mL |
100 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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5% DMSO+30% PEG300+5% Tween 80+60% 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 50 μL DMSO (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:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Rizatriptan benzoate 145202-66-0 GPCR/G Protein Neuroscience 5-HT Receptor MK 462 Rizatriptan Rizatriptan Benzoate MK 462 Benzoate inhibit 苯甲酸利扎曲坦 MK-462 Benzoate Inhibitor MK462 5-hydroxytryptamine Receptor MK-462 Serotonin Receptor MK462 Benzoate inhibitor