- GW788388
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- $58.00
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2026-07-27
- CAS:452342-67-5
- Purity: 99.58%
- Supply Ability: 10g
- GW788388
-
-
2026-07-06
- CAS:452342-67-5
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 20Tons
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| | GW788388 Basic information |
| Product Name: | GW788388 | | Synonyms: | 4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide;N-(oxan-4-yl)-4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}benzaMide;GW 788388 4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide;GW 788388;BenzaMide, 4-[4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-;4-(4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)pyridin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)benzamide;GW788388;GW 788388;GW 788388, >=98% | | CAS: | 452342-67-5 | | MF: | C25H23N5O2 | | MW: | 425.48 | | EINECS: | | | Product Categories: | Inhibitors;Smad;TGF-beta | | Mol File: | 452342-67-5.mol |  |
| | GW788388 Chemical Properties |
| density | 1.34 | | storage temp. | 2-8°C | | solubility | Soluble in DMSO (18 mg/ml with warming) | | form | solid | | color | Off-white | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| | GW788388 Usage And Synthesis |
| Description | 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. | | Uses | GW788388 is a new TGF-beta type I receptor inhibitor with a much improved pharmacokinetic profile compared with SB431542. | | in vivo | GW788388 given orally for 5 weeks significantly reduces renal fibrosis and decreased the mRNA levels of key mediators of extracellular matrix deposition in kidneys in db/db mice[1]. GW788388 (50 mg/kg/day, p.o.) significantly attenuates systolic dysfunction in the MI animals, together with the attenuation of the activated (phosphorylated) Smad2 (P < 0.01), α-smooth muscle actin (P < 0.001), and collagen I (P < 0.05) in the noninfarct zone of MI rats[2]. GW788388 reduces the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). GW788388 significantly reduces the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis[3]. | | storage | Store at +4°C | | References | [1] FRANÇOISE GELLIBERT. Discovery of 4-{4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): A Potent, Selective, and Orally Active Transforming Growth Factor-β Type I Receptor Inhibitor[J]. Journal of Medicinal Chemistry, 2006, 49 7: 2210-2221. DOI:10.1021/jm0509905
[2] M. PETERSEN . Oral administration of GW788388, an inhibitor of TGF-β type I and II receptor kinases, decreases renal fibrosis[J]. Kidney international, 2008, 73 6: Pages 705-715. DOI:10.1038/sj.ki.5002717
[3] FABIANE L DE OLIVEIRA. Oral administration of GW788388, an inhibitor of transforming growth factor beta signaling, prevents heart fibrosis in Chagas disease.[J]. PLoS Neglected Tropical Diseases, 2012: e1696. DOI:10.1371/journal.pntd.0001696
[4] KAZUHIRO NOMA . The Essential Role of Fibroblasts in Esophageal Squamous Cell Carcinoma–Induced Angiogenesis[J]. Gastroenterology, 2008, 134 7: Pages 1981-1993. DOI:10.1053/j.gastro.2008.02.061
[5] YUNMEE LHO. Effects of TGF-β1 Receptor Inhibitor GW788388 on the Epithelial to Mesenchymal Transition of Peritoneal Mesothelial Cells.[J]. International Journal of Molecular Sciences, 2021, 22 9. DOI:10.3390/ijms22094739 |
| | GW788388 Preparation Products And Raw materials |
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