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CAS No.: 1619931-27-9

Seralutinib Catalog No. CSN27849

Synonyms: GB002;PK10571

Seralutinib is a potent and novel inhaled PDGFR inhibitor, used in the study for pulmonary arterial hypertension.

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技术信息

生物活性

描述Platelet-derived growth factor (PDGF) was discovered as a serum-derived component necessary for the growth of smooth muscle cells, fibroblasts, and glial cells. Although PDGF signaling is most closely associated with mesenchymal cells, PDGFs and PDGF receptors are widely expressed in the mammalian central nervous system^[2]. Today the PDGF family of growth factors consists of five different disulphide-linked dimers built up of four different polypeptide chains encoded by four different genes. These isoforms, PDGF-AA, PDGF-AB, PDGF-BB, PDGF-CC and PDGF-DD, act via two receptor tyrosine kinases, PDGF receptors alpha and beta^[3]. PDGFRα expression decreases with adipocyte lineage, while PDGFRβ inhibits white adipocyte differentiation. In addition, PDGFRβ induces proliferation, migration, and angiogenesis and up-regulates the expression of paracrine factors in adipose-derived stem cells(ASCs)^[4].Overactivity of PDGF receptor signaling, by overexpression or mutational events, may drive tumor cell growth. In addition, pericytes of the vasculature and fibroblasts and myofibroblasts of the stroma of solid tumors express PDGF receptors, and PDGF stimulation of such cells promotes tumorigenesis^[5]. Seralutinib(GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.GB002 dose-and time-dependently induces lung BMPR2 protein expression.GB002-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1298 mL
- 10.6488 mL
- 21.2977 mL
- 5 mM
- 0.4260 mL
- 2.1298 mL
- 4.2595 mL
- 10 mM
- 0.2130 mL
- 1.0649 mL
- 2.1298 mL

技术信息

CAS号	1619931-27-9	储存条件	粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C27H27N5O3	运输	蓝冰
分子量	469.54	别名	GB002;PK10571

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