Solifenacin|242478-37-1|(索利那新; YM905 free base)-陌孚医药/Medlife

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Solifenacin (Synonyms: 索利那新; YM905 free base)

目录号: PL06857 纯度: ≥99%

CAS No. :242478-37-1

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中文名称	Solifenacin
中文别名	索非那新;1-氮杂双环[2.2.2]辛烷-8-基-(1S)-1-苯基-3,4-二氢-1H-异喹啉-2-甲酸酯;(8R)-1-氮杂双环(2.2.2)辛烷-8-基-(1S)-1-苯基-3,4-二氢-1H-异喹啉-2-甲酸酯 (索非那新);索非那新杂质;索菲那新;索利那新;索利那新-D5
英文名称	Solifenacin
英文别名	Solifenacin;[(8R)-1-azabicyclo[2.2.2]octan-8-yl] (1S)-1-phenyl-3,4-dihydro-1H-isoquinoline-2-carboxylate;Solifenacin intermediate;YM905;(1S)-(3R)-1-azabicyclo[2,2,2]oct-3-yl-3,4-dihydro-1-phenyl-2(1H)-isoquinoline carboxylate;(1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate;(1S,3'R)-quinuclidin-3'-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate;2(1H)-Isoquinolinecarboxylic acid,3,4-dihydro-1-phenyl-,1-azabicyclo(2.2.2)oct-3-yl ester,(R-(R,S));3,4-dihydro-1-phenyl-(1S)-2(1H)-Isoquinolinecarboxylic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester;Unii-A891
Cas No.	242478-37-1
分子式	C₂₃H₂₆N₂O₂
分子量	362.47
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Solifenacin (YM905 free base) 是一种新型的毒蕈碱受体 (muscarinic receptor) 拮抗剂，对 M₁，M₂ 和 M₃ 受体的 pK_i 值分别为 7.6, 6.9 和 8.0。

生物活性

Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pK i s of 7.6, 6.9 and 8.0 for M 1 , M 2 and M 3 receptors, respectively.

性状

Solid

IC50 & Target[1][2]

pKi: 7.6 (M1 receptor), 6.9 (M2 receptor), 8.0 (M3 receptor)

体外研究(In Vitro)

Solifenacin is a novel muscarinic receptor antagonist with pKis of 7.6±0.056, 6.9±0.034 and 8.0±0.021 for M1, M2 and M3 receptors, respectively. In murine submandibular gland cells, the antagonistic effects of 100 nM Solifenacin and oxybutynin on Ca mobilization evoked by varying doses of carbachol (CCh) are examined. Solifenacin does not shift the CCh dose-activation curve in a parallel manner whereas oxybutynin shows insurmountable antagonism. The pKb values are obtained as 7.4±0.17 for Solifenacin and 8.8±0.21 for oxybutynin. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Solifenacin reduces bladder responses by 40% at a dose of 210 nmol/kg (0.1 mg/kg) and abolishes them at 2100 nmol/kg (1 mg/kg). In contrast, its inhibitory effects on salivary and cardiac responses are only slight at 630 nmol/kg (0.3 mg/kg), and reach 66% and 49%, respectively, at 2100 nmol/kg (1 mg/kg). At doses of 63 and 210 nmol/kg (0.03 and 0.1 mg/kg), Solifenacin slightly increases saliva secretion. Solifenacin (0.01 to 0.3 mg/kg i.v.) dose-dependently increases bladder capacity and voided volume at doses of 0.03 mg/kg i.v. or more, but does not affect residual volume or micturition pressure at any dose tested. 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

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Ikeda K, et al. M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland. Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):97-103.
[2]. Suzuki M, et al. Effects of solifenacin succinate (YM905) on detrusor overactivity in conscious cerebral infarctedrats. Eur J Pharmacol. 2005 Apr 4;512(1):61-6.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (137.95 mM)H₂O : < 0.1 mg/mL (insoluble)

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产品使用指南

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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