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GW788388

Product Name
GW788388
CAS No.
452342-67-5
Chemical Name
GW788388
Synonyms
CS-59;GW 788388;GW 788388, >=98%;GW788388 USP/EP/BP;GW788388;GW 788388;GW788388, 10 mM in DMSO;N-(oxan-4-yl)-4-[4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridin-2-yl]benzamide;N-(oxan-4-yl)-4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}benzaMide;4-[4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl]-N-(tetrahydropyran-4-yl)benzamide;4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
CBNumber
CB42514620
Molecular Formula
C25H23N5O2
Formula Weight
425.48
MOL File
452342-67-5.mol
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GW788388 Property

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.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16255
Product name
GW 788388
Purity
≥98%
Packaging
1mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
16255
Product name
GW 788388
Purity
≥98%
Packaging
5mg
Price
$104
Updated
2024/03/01
Cayman Chemical
Product number
16255
Product name
GW 788388
Purity
≥98%
Packaging
10mg
Price
$166
Updated
2024/03/01
Cayman Chemical
Product number
16255
Product name
GW 788388
Purity
≥98%
Packaging
25mg
Price
$315
Updated
2024/03/01
Tocris
Product number
3264
Product name
GW788388
Purity
≥98%(HPLC)
Packaging
10
Price
$259
Updated
2021/12/16
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GW788388 Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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GW788388 Suppliers

Canada 1 China 145 India 2 United Kingdom 1 United States 16 Global 165
Tocris Bioscience
Tel
--
Fax
--
Email
customerservice@tocris.co.uk
Country
United Kingdom
ProdList
5726
Advantage
77

452342-67-5, GW788388Related Search:

GW284543 GW9662 GW441756 GW5074 SB 431542 LY2109761 ALK5 inhibitor II Dabrafenib SB525334 LY 2157299 AZ20 Ibrutinib KU57788(NU7441) GW 284543 hydrochloride - UNC 10225170 hydrochloride 5-[3-Methoxy-4-(4-methoxy-benzyloxy)-benzyl]-pyrimidine-2,4-diamine GW9508 2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]- N-Eicosanoyl Serotonin

  • 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%
  • CS-59
  • 4-[4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-2-pyridinyl]-N-(tetrahydro-2H-pyran-4-yl)-benzamide
  • GW788388 USP/EP/BP
  • GW788388, 10 mM in DMSO
  • N-(oxan-4-yl)-4-[4-(5-pyridin-2-yl-1H-pyrazol-4-yl)pyridin-2-yl]benzamide
  • 452342-67-5
  • 45324-67-5
  • Inhibitors
  • Smad
  • TGF-beta