GW788388

Bezeichnung:GW788388

CAS-Nr452342-67-5

Englisch Name:GW788388

CBNumberCB42514620

SummenformelC25H23N5O2

Molgewicht425.48

MOL-Datei452342-67-5.mol

GW788388 physikalisch-chemischer Eigenschaften

Dichte	1.34
storage temp.	2-8°C
Löslichkeit	Soluble in DMSO (18 mg/ml with warming)
Aggregatzustand	solid
Farbe	Off-white
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Gefahreninformationscode (GHS)

GW788388 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC₅₀ = 18 nM). It inhibits the expression of collagen type I in cells (IC₅₀ = 93 nM) and in mice when given orally at 10 mg/kg once a day. As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I. GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro. Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.
Verwenden
GW788388 is a new TGF-beta type I receptor inhibitor with a much improved pharmacokinetic profile compared with SB431542.
Lager
Store at +4°C
Einzelnachweise
Gellibert et al. (2006), Discovery of 4-{4-[3-(pyridine-2-yl)-1H-pyrazol-4-yl}pyridine-2-yl}-N-(tetrahydro-2H-pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor; J. Med. Chem. 49 2210 Petersen et al. (2008), Oral administration of GW788388, an inhibitor of TGF-beta type I and II receptor kinases, decreases renal fibrosis; Kidney Int. 73 705 De Oliveira et al. (2012), Oral administration of GW788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in Chagas disease; PLoS Negl. Trop. Dis. 6 e1696 Noma et al. (2008), The essential role of fibroblasts in esophageal squamous cell carcinoma-induced angiogenesis; Gastroenterology. 134 1981 Lho et al. (2021), Effects of TGF-? Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells; Int. J. Mol. Sci. 22 4739

GW788388 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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