Fesoterodine L-mandelate|1206695-46-6|(弗斯特罗定扁桃酸盐；非索罗定扁桃酸盐)-陌孚医药/Medlife

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Fesoterodine L-mandelate (Synonyms: 弗斯特罗定扁桃酸盐；非索罗定扁桃酸盐)

目录号: PL06841 纯度: ≥98%

CAS No. :1206695-46-6

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中文名称	Fesoterodine L-mandelate
中文别名	2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxy-methylphenyl isobutyrate mandelate;Fesoterodine ((S)-2-hydroxy-2-phenylacetic acid)
英文名称	Fesoterodine L-mandelate
英文别名	Fesoterodine ((S)-2-hydroxy-2-phenylacetic acid);2-[(1R)-3-[bis(1-methylethyl)amino]-1-phenylpropyl]-4-hydroxy-methylphenyl isobutyrate mandelate;[2-[3-[Di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate;2-hydroxy-2;Fesoterodine L-mandelate;Fesoterodine (L-mandelate);[2-[(1R)-3-[di(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate;(2S)-2-hydroxy-2-phenylacetic acid;C12774
Cas No.	1206695-46-6
分子式	C₃₄H₄₅NO₆
分子量	563.72
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

Fesoterodine L-mandelate 是一种口服有效，非亚型选择性的，竞争性毒蕈碱受体 (mAChR) 拮抗剂，对 M1，M2，M3，M4，M5 受体的 pK_i 值分别为 8.0，7.7，7.4，7.3，7.5。Fesoterodine L-mandelate 用于膀胱过度活动症 (OAB)。

生物活性

Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB).

性状

Solid

IC50 & Target[1][2]

pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)

体外研究(In Vitro)

Fesoterodine L-mandelate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition.
After oral administration, Fesoterodine L-mandelate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine).
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Fesoterodine L-mandelate (0.01-1 mg/kg; IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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]. Ellsworth P, et al. Fesoterodine for the treatment of urinary incontinence and overactive bladder. Ther Clin Risk Manag. 2009;5:869-76. Epub 2009 Nov 18.
[2]. Didem Yilmaz-Oral, et al. The Beneficial Effect of Fesoterodine, a Competitive Muscarinic Receptor Antagonist on Erectile Dysfunction in Streptozotocin-induced Diabetic Rats

溶解度数据	In Vitro: DMSO : 100 mg/mL (177.39 mM; Need ultrasonic)配制储备液

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Data Sheet

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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