Berotralstat (Synonyms: BCX7353)
目录号: PL11214 纯度: ≥98%
CAS No. :1809010-50-1
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中文名称
Berotralstat
英文名称
Berotralstat
英文别名
Berotralstat;XZA0KB1BDQ;BCX7353;Berotralstat (USAN);Berotralstat [USAN];1-[3-(aminomethyl)phenyl]-N-(5-{(R)-(3-;cyanophenyl)[(cyclopropylmethyl)amino]methyl}-2-;fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-;Orladeyo;Berotralstat [INN];Berotralstat [USAN:INN];GTPL11347;WHO 10907;D11673;1-(3-(Aminomethyl)phenyl)-N-(5-((R)-(3-cyanophenyl)((cyclopropylmethyl)amino)methyl)-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide;1H-pyrazol
Cas No.
1809010-50-1
分子式
C30H26F4N6O
分子量
562.56
包装储存
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
产品详情
Berotralstat (BCX7353) 是一种低毒性,有效,高特异性,第二代,具有口服活性的 plasma kallikrein 抑制剂,用于遗传性血管水肿 (hereditary angioedema,HAE) 的研究。 Berotralstat 通过阻断 plasma kallikrein 释放缓激肽的酶活性来发挥作用,缓激肽是促进与 HAE 发作相关的肿胀和疼痛的主要生物肽。
生物活性
Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
性状
Solid
IC50 & Target[1][2]
Plasma kallikrein
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
ClinicalTrial
参考文献
[1]. Zuraw B, et al. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial [published online ahead of print, 2020 Oct 21]. J Allergy Clin Immunol. 2020;S0091-6749(20)31484
[2]. Manning ME, et al. Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies. Allergy Asthma Proc. 2021;42(4):274-282.
溶解度数据
In Vitro: DMSO : 100 mg/mL (177.76 mM; Need ultrasonic)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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