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GW-6604, an ALK5 inhibitor, exhibits clear antifibrotic effects leading to improved liver function.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 28 € | In Stock | |
5 mg | 69 € | In Stock | |
10 mg | 112 € | In Stock | |
25 mg | 186 € | In Stock | |
50 mg | 278 € | In Stock | |
100 mg | 405 € | In Stock |
Description | GW-6604, an ALK5 inhibitor, exhibits clear antifibrotic effects leading to improved liver function. |
In vitro | GW-6604 inhibited autophosphorylation of ALK5 with an IC50 of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC50 = 500 nM)[2]. |
In vivo | GW-6604 (40 mg/kg p.o.) increased liver regeneration in TGF-beta-overexpressing mice, which had undergone partial hepatectomy. In an acute model of liver disease, GW-6604 reduced by 80% the expression of collagen IA1. In a chronic model of DMN-induced fibrosis where DMN was administered for 6 weeks and GW-6604 dosed for the last 3 weeks (80 mg/kg p.o., b.i.d.), mortality was prevented and DMN-induced elevations of mRNA encoding for collagen IA1, IA2, III, TIMP-1 and TGF-beta were reduced by 50-75%. Inhibition of matrix genes overexpression was accompanied by reduced matrix deposition and reduction in liver function deterioration, as assessed by bilirubin and liver enzyme levels[2]. |
Molecular Weight | 298.34 |
Formula | C19H14N4 |
Cas No. | 452342-37-9 |
Smiles | c1[nH]nc(c1-c1ccnc(c1)-c1ccccc1)-c1ccccn1 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 2.98 mg/mL (10 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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