Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fesoterodine fumarate (Toviaz) 是可口服的,非亚型选择性的竞争性毒蕈碱受体拮抗剂,用于膀胱过度活动症,对 M1、M2、M3、M4 和 M5 受体的pKi 值分别为 8.0、7.7、7.4、7.3 和 7.5。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 497 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,290 | 现货 | ||
50 mg | ¥ 1,860 | 现货 | ||
100 mg | ¥ 2,680 | 现货 | ||
500 mg | ¥ 5,180 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 577 | 现货 |
产品描述 | Fesoterodine fumarate (Toviaz) is the fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyl tolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine. |
体外活性 | Fesoterodine is rapidly and extensively converted to 5-HMT, such that the pharmacologic activity appears to be primarily attributable to 5-HMT. [1] Fesoterodine is a competitive antagonist of cholinergic agonist-stimulated responses in human M1-M5 cell lines and has a similar potency and selectivity profile to the radioligand-binding studies. Fesoterodine causes a rightward shift of the concentration-response curve for carbachol with no depression of the maximum in rat bladder strips, and concentration-dependently reduces contractions induced by electrical field stimulation (EFS). [2] Fesoterodine is hydrolyzed by nonspecific esterases to 5-hydroxmethyl tolterodine (5-HMT), which is the active metabolite and is responsible for all its antimuscarinic activity. [3] |
别名 | Toviaz, SPM 907, 富马酸非索罗定 |
分子量 | 527.65 |
分子式 | C26H37NO3·C4H4O4 |
CAS No. | 286930-03-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (176.3 mM)
H2O: 92 mg/mL (174.4 mM)
Ethanol: 93 mg/mL (176.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O / Ethanol | 1 mM | 1.8952 mL | 9.476 mL | 18.952 mL | 47.3799 mL |
5 mM | 0.379 mL | 1.8952 mL | 3.7904 mL | 9.476 mL | |
10 mM | 0.1895 mL | 0.9476 mL | 1.8952 mL | 4.738 mL | |
20 mM | 0.0948 mL | 0.4738 mL | 0.9476 mL | 2.369 mL | |
50 mM | 0.0379 mL | 0.1895 mL | 0.379 mL | 0.9476 mL | |
100 mM | 0.019 mL | 0.0948 mL | 0.1895 mL | 0.4738 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。
Fesoterodine fumarate 286930-03-8 Neuroscience AChR 5-HMT antimuscarinic SPM-907 muscarinic mAChR overactive Fesoterodine Fumarate inhibit OAB Fesoterodine receptor SPM7605 Muscarinic acetylcholine receptor bladder Toviaz SPM 907 Desfesoterodine SPM907 Inhibitor 富马酸非索罗定 orally inhibitor