Solabegron (Synonyms: GW 427353)
目录号: PL14274 纯度: ≥99%
CAS No. :252920-94-8
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中文名称
Solabegron
英文名称
Solabegron
英文别名
[1,1'-Biphenyl]-3-carboxylicacid, 3'-[[2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]ethyl]amino]-;GW 427353;Solabegron;GW427353;(R)-3'-((2-((2-(3-Chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)-[1,1'-biphenyl]-3-carboxylic acid;55P6YH9O6N;C23H23ClN2O3;(R)-3'-((2-((2-(3-chlorophenyl)-2-hydroxyethyl)amino)ethyl)amino)-(1,1'-biphenyl)-3-carboxylic acid;Solabegron [INN];solabegronum;(R)-3'-[[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]amino]ethyl]amino]-[1,1'-biphenyl]-3-carboxylic acid;GTPL9512;CHEB
Cas No.
252920-94-8
分子式
C23H23ClN2O3
分子量
410.89
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
Solabegron (GW 427353) 是 β3 肾上腺素能受体 (β3-AR) 的选择性激动剂, 在中国仓鼠卵巢细胞中测得的 EC50 值为22 nM。可用于膀胱过度活跃和肠易激综合征的研究。
生物活性
Solabegron (GW 427353) is a selective β 3 -adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β 3 -AR, with an EC 50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
性状
Solid
IC50 & Target[1][2]
EC50: 22 nM (β3-AR in cells).
体内研究(In Vivo)
Solabegron (GW427353) at 3 mg/kg i.v. evokes an increase in micturition volume threshold that prevented the acetic acid-evoked decreases in dogs. The low dose (1 mg/kg) shows no significant activity. 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, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
ClinicalTrial
参考文献
[1]. Hicks A, et al. GW427353 (solabegron), a novel, selective beta3-adrenergic receptor agonist, evokes bladder relaxation and increases micturition reflex threshold in the dog. J Pharmacol Exp Ther. 2007 Oct;323(1):202-9.
[2]. Andersson KE, et al. Selective β3-adrenoceptor agonists for the treatment of overactive bladder. J Urol. 2013 Oct;190(4):1173-80.
溶解度数据
In Vitro: DMSO : ≥ 33.33 mg/mL (81.12 mM)配制储备液
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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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