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。
货号:ajcx33080
CAS:1619931-27-9
分子式:C27H27N5O3
分子量：469.53
溶解度:DMSO : 100 mg/mL (212.98 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension[1].

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[1].GB002-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation[2].GB002 dose- and time-dependently induces lung BMPR2 protein expression[2].

[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).