Seralutinib (Synonyms: GB002; PK10571) |
| رقم الكتالوجGC62114 |
سيرالوتينيب (GB002) هو مثبط PDGFRα و PDGFRβ عن طريق الاستنشاق
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Cas No.: 1619931-27-9
Sample solution is provided at 25 µL, 10mM.
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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).
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