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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride

产品编号 T40161 CAS 250214-40-5

别名: (Rac)-5-Hydroxymethyl Tolterodine hydrochloride, (Rac)-PNU-200577hydrochloride, (Rac)-Desfesoterodine hydrochloride

(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions.

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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride Chemical Structure

(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, CAS 250214-40-5

规格	价格/CNY		货期	数量
2 mg	￥ 1,150		5日内发货

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(Rac)-5-Hydroxymethyl Tolterodine hydrochloride 的其他形式现货产品:

Desfesoterodine

其他形式的 (Rac)-5-Hydroxymethyl Tolterodine hydrochloride:

Desfesoterodine
现货
(Rac)-5-Hydroxymethyl Tolterodine
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, also known as (Rac)-Desfesoterodine hydrochloride, is an active metabolite of Tolterodine that functions as a mAChR antagonist. It exhibits significant affinity (K i values) for M1, M2, M3, M4, and M5 receptors, with values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM, respectively. This compound is commonly employed in research related to overactive bladder conditions.
体外活性	In vitro, (Rac)-5-Hydroxymethyl Tolterodine (PNU-200577) hydrochloride produces a competitive and concentration-dependent inhibition of carbachol-induced contraction of guinea-pig isolated urinary bladder strips (K B of 0.84 nM; pA2 of 9.14)[2].
体内活性	(Rac)-5-Hydroxymethyl Tolterodine (5-HMT; 0.88 μmol/kg; i.v.) hydrochloride treatment shows the binding activity of (Rac)-5-Hydroxymethyl Tolterodine hydrochloride to muscarinic receptors is significantly observed in all tissues, except cerebral cortex, with a longer duration in bladder[3].

别名	(Rac)-5-Hydroxymethyl Tolterodine hydrochloride, (Rac)-PNU-200577hydrochloride, (Rac)-Desfesoterodine hydrochloride
分子量	377.95
分子式	C22H32ClNO2
CAS No.	250214-40-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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. 3. Shizuo Yamada, et al. Muscarinic receptor binding of fesoterodine, 5-hydroxymethyl tolterodine, and tolterodine in rat tissues after the oral, intravenous, or intravesical administration. J Pharmacol Sci. 2019 May;140(1):73-78.

剂量换算

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体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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