Seralutinib (Synonyms: GB002; PK10571)
目录号: PL08995 纯度: ≥99%
CAS No. :1619931-27-9
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中文名称
Seralutinib
英文名称
Seralutinib
英文别名
3P63ZTE3OY;SB17246;3-Pyridinecarboxamide, N-(3-((1S)-1-((6-(3,4-dimethoxyphenyl)-2-pyrazinyl)amino)ethyl)phenyl)-5-methyl-;Unii-3P63zte3OY;Seralutinib
Cas No.
1619931-27-9
分子式
C27H27N5O3
分子量
469.54
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Seralutinib (GB002) 是一个可吸入的 PDGFRα 和 PDGFRβ 激酶抑制剂。Seralutinib (GB002) 可用于肺动脉高压的研究。
生物活性
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
性状
Solid
体内研究(In Vivo)
Seralutinib (GB002) (two-week treatment, delivered by inhalation) significantly reduces right ventricular systolic pressure and mean pulmonary artery pressure. Hemodynamic changes are accompanied by reduced pulmonary arteriole muscularization and restoration of BMPR2 protein expression in the lung lobes in Seralutinib (GB002)-treated animals. Seralutinib (GB002) is well tolerated.
GB002-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation.
GB002 dose- and time-dependently induces lung BMPR2 protein expression.
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]. Anna Galkin, et al. Abstract 11102: Gb002, A Novel Inhaled Pdgfr Kinase Inhibitor, Demonstrates Efficacy in the Su5416 Hypoxia Rat Model of Pulmonary Arterial Hypertension (pah). Circulation. 2019;140:A11102.
[2]. Anna Galkin, et al. Pharmacologic Characterization of GB002, a Novel Inhaled PDGFR Kinase Inhibitor in Development for Pulmonary Arterial Hypertension (PAH).
溶解度数据
In Vitro: DMSO : 100 mg/mL (212.98 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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