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- Fesoterodine fumarate 286930-03-8

- Fesoterodine fumarate 286930-03-8
Fesoterodine fumarate 286930-03-8
产品描述 描述 Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder基本信息 别名 富马酸非索罗定外观 白色至类白色固体可溶性/溶解性
DMSO : 93 mg/mL (176.3 mM)
Ethanol : 93 mg/mL (176.3 mM)
Water : 92 mg/mL (174.4 mM)生物活性 靶点 AChRIn vitro(体外研究) Fesoterodine is rapidly and extensively converted to 5-HMT, such that the pharmacologic activity appears to be primarily attributable to 5-HMT. 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). 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.参考文献 参考文献 1. Malhotra B, et al. Curr Med Chem, 2009, 16(33), 4481-4489.
2. Ney P, et al. BJU Int, 2008, 101(8), 1036-1042.
3. Vella M, et al. Expert Opin Drug Saf, 2011, 10(5), 805-808.
研究领域 研究领域 NeuroscienceDrug DiscoverySmall Molecule DrugLead Compound DiscoveryFesoterodine fumarate 286930-03-8温馨提示:本产品仅作科研实验使用,不支持临床等研究
