Tolterodine tartrate

(Synonyms: Kabi-2234; PNU-200583E)
目录号: PL06850 纯度: ≥99%
Tolterodine Tartrate (Kabi-2234; PNU-200583E) 是一种有效的毒蕈碱受体拮抗剂,体内对膀胱具有选择性。
CAS No. :124937-52-6
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中文名称
Tolterodine tartrate
中文别名
酒石酸托特罗定;酒石酸托特罗定 酒石酸托特罗定中间体;酒石酸托特罗;(1R,2R)-N,N-二-对-甲苯磺酰-1,2-二苯基-1,2-乙烯二胺;酒石酸托特罗定 USP标准品;酒石酸托特罗定 标准品;托特罗定;L-酒石酸托特罗定;酒石酸托特罗定-D14;酒石酸托特罗定(标准品);(R)-2-[1-苯基-3-(二异丙基氨基)丙基]-4-甲基苯酚-L-酒石酸盐
英文名称
Tolterodine tartrate
英文别名
(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,3R)-2,3-dihydroxysuccinate;DETROL;DETRUSITOL;PNU-20058E;(+)-(R)-2-[A-[2-(DIISOPROPYLAMINO) ETHYL]BENZYL]-P-CRESOL TARTRATE;TOLTERODINE L-TARTRATE;(R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine L-hydrogen tartrate;R-(+)-N,N-Diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine, PNU-20058E, Detrol, Detrusitol, R-(+)-Toltaridine;TOLERODINETARTRATE;Tolterodine tartrate;(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-methylphenol 2,3-dihydroxysuccinate;Tolterodine (as Tartrate);Tolterodine (tartrate);Tolterodine L-Tartra;(+)-R)-2-{A-[2-(DIISOPROPYLAMINO)ETHYL]BENZYL}-P-CRESOL TARTRATE;(R)-2-(3-(Diisopropylamino)-1-phenylpropyl)-4-methylphenol (2R,;(R)-2-(3-DIISOPROPYLAMINO-1-PHENYL-PROPYL)-4-METHYL-PHENOL L-TARTRATE;(R)-2-(3-Diisopropylamino-1-phenyl-propyl)-p-cresol L-tartrate;TOLTERODINE;(R)-Tolterodine L-tartrate;Detrol LA;PNU-200583E;Tolterodine(Detrol);Tolterodine Tartrate API
Cas No.
124937-52-6
分子式
C22H31NO.C4H6O6
分子量
475.57
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)
详情描述
Tolterodine Tartrate (Kabi-2234; PNU-200583E) 是一种有效的毒蕈碱受体拮抗剂,体内对膀胱具有选择性。
产品详情
Tolterodine Tartrate (Kabi-2234; PNU-200583E) 是一种有效的毒蕈碱受体拮抗剂,体内对膀胱具有选择性。
生物活性
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
性状
Solid
体外研究(In Vitro)
Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Tolterodine was extensively metabolized in vivo. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased. 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)
ClinicalTrial
参考文献
[1]. Nilvebrant L. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7.
[2]. Andersson SH, et al. Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs. Drug Metab Dispos. 1998 Jun;26(6):528-35.
溶解度数据
In Vitro: DMSO : 100 mg/mL (210.27 mM; Need ultrasonic)H2O : 16.67 mg/mL (35.05 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Nilvebrant L. Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7.
[2]. Andersson SH, et al. Biotransformation of tolterodine, a new muscarinic receptor antagonist, in mice, rats, and dogs. Drug Metab Dispos. 1998 Jun;26(6):528-35.

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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