(Rac)-5-Hydroxymethyl Tolterodine (Synonyms: (Rac)-Desfesoterodine; (Rac)-PNU-200577)
目录号: PL06869
CAS No. :200801-70-3
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中文名称
(Rac)-5-Hydroxymethyl Tolterodine
中文别名
2,8-双(三氟甲基)喹啉-4-羧酸;5-羟甲基托特罗定;5-羟甲托特罗定;5-羟甲托特罗定-d5;苯甲醇, 3-[3-[双(1-甲基乙基)氨基]-1-苯基丙基]-4-羟基-;弗斯特罗定杂质A;3-[3-[二异丙基氨基]-1-苯基丙基]-4-羟基-苯甲醇
英文名称
(Rac)-5-Hydroxymethyl Tolterodine
英文别名
2-(3-(Diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol;2-[3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenol;3-[3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxybenzenemethanol;Tolterodine 5-Hydroxymethyl (racemate, as HCl salt);(R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol;2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol;feso deacyl raceme;N,N-diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropylamine;rac 5-Hydroxymethyl Tolterodine;RS-N,N-diisopropyl-3-(2-hydroxy-5-(hydroxymethyl)phenyl)-3-phenylpropylamine;C22H31NO2;2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol;DUXZAXCGJSBGDW-UHFFFAOYSA-N;5-Hydroxy Tolterodine;(+)-N,N-Diisopropyl-3-(2-hydroxy-5-hydroxymethylphenyl)-3-phenylpropylamine;HMS3656F09;racemic 5-hyd
Cas No.
200801-70-3
分子式
C22H31NO2
分子量
341.49
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) 是 Tolterodine 的一种活性代谢物,是一种 mAChR 拮抗剂 (M1、M2、M3、M4 和 M5 受体的 Ki 值分别为 2.3 nM、2 nM、2.5 nM、2.8 nM 和 2.9 nM)。(Rac)-5-Hydroxymethyl Tolterodine 可用于膀胱过度活动症研究。
生物活性
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (K i values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research.
性状
Solid
IC50 & Target[1][2]
Ki: M1 (2.3 nM), M2 (2 nM), M3 (2.5 nM), M4 (2.8 nM), and M5 (2.9 nM)
体外研究(In Vitro)
In vitro, (Rac)-5-Hydroxymethyl Tolterodine (PNU-200577) produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips (KB of 0.84 nM; pA2 of 9.14). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
(Rac)-5-Hydroxymethyl Tolterodine (5-HMT; 0.88 μmol/kg; i.v.) treatment shows the binding activity of (Rac)-5-Hydroxymethyl Tolterodine to muscarinic receptors is significantly observed in all tissues, except cerebral cortex, with a longer duration in bladder. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. L Nilvebrant, et al. Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol. 1997 Oct;81(4):169-72.
[2]. B Malhotra, et al. The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9.
溶解度数据
In Vitro: DMSO : 100 mg/mL (292.83 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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