Dabuzalgron (Synonyms: Ro 115-1240)
目录号: PL14271 纯度: ≥98%
CAS No. :219311-44-1
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中文名称
Dabuzalgron
中文别名
达布扎琼;N-[6-氯-3-[(4,5-二氢-1H-咪唑-2-基)甲氧基]-2-甲基苯基]甲磺酰胺
英文名称
Dabuzalgron
英文别名
Dabuzalgron;N-[6-Chloro-3-[(4,5-dihydro-1H-imidazol-2-yl)methoxy]-2-methylphenyl]methanesulfonamide;N-[6-chloro-3-(4,5-dihydro-1H-imidazol-2-ylmethoxy)-2-methylphenyl]methanesulfonamide;Ro-115-1240;UNII-LGX4GZ74WO;N-(6-Chloro-3-((4,5-dihydro-1H-imidazol-2-yl)methoxy)-2-methylphenyl)methanesulfonamide;LGX4GZ74WO;n-(6-chloro-3-((4,5-dihydro-1H-imidazol-2-yl)methoxy)-2-methyl phenyl)methanesulfonamide;Dabuzalgron [INN];dabuzalgronum;GTPL3469;BDBM50377398;Ro 11
Cas No.
219311-44-1
分子式
C12H16ClN3O3S
分子量
317.79
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Dabuzalgron (Ro 115-1240) 是一种口服活性的,选择性的 α-1A 肾上腺素能受体激动剂,动物模型中,用于缓解尿失禁。Dabuzalgron 可通过维持线粒体功能来预防由阿霉素引起的心脏毒性。
生物活性
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.
性状
Solid
IC50 & Target[1][2]
α-1A adrenergic receptor
体外研究(In Vitro)
Dabuzalgron treatment increases ERK phosphorylation in a dose-dependent fashion with an EC50 of 4.8 μM. ERK1/2 activation contributes to the cardioprotective effects of Dabuzalgron.
Dabuzalgron (10 μM; 4 hours) protects NRVMs from cell death due to Doxorubicin (DOX).
Activation of the α1A-AR with Dabuzalgron (10 μM; 4 hours) mitigates the detrimental effects of DOX on mitochondrial membrane potential and abrogates the activation of important elements of the apoptotic response to mitochondrial damage. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Dabuzalgron (10 μg/kg; oral gavage; twice daily; for 7 days; C57Bl6J wild-type or α1A-AR knockout mice) treatment protects against DOX cardiotoxicity by activating the α1A-AR. Dabuzalgron protects against the reduction in transcripts related to mitochondrial function, up-regulates PGC1α, preserves ATP content, and reduces oxidative stress in the hearts of mice treated with DOX. 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
参考文献
[1]. Beak J, et al. An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity. JACC Basic Transl Sci. 2017 Feb;2(1):39-53.
溶解度数据
In Vitro: DMSO : 26 mg/mL (81.82 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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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