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GKT137831

Chemical Structure : GKT137831

CAS No.: 1218942-37-0

GKT137831 (Setanaxib, GKT-137831, GKT831)

Catalog No.: PC-42961Not For Human Use, Lab Use Only.

GKT137831 (Setanaxib, GKT-137831) is a potent, selective, dual NADPH oxidase Nox1/4 inhibitor with Ki of 110/140 nM, 15-fold less potent on Nox2 and 3-fold less potent on Nox5, and no affinity for xanthine oxidase.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GKT137831 (Setanaxib, GKT-137831) is a potent, selective, dual NADPH oxidase Nox1/4 inhibitor with Ki of 110/140 nM, 15-fold less potent on Nox2 and 3-fold less potent on Nox5, and no affinity for xanthine oxidase.
GKT137831 (Setanaxib) attenuates liver fibrosis and ROS production in both SOD1mu and WT mice, suppresses ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT in hepatic stellate cells (HSCs).

Physicochemical Properties

M.Wt 394.8542
Formula C21H19ClN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 37 mg/mL

Chemical Name/SMILES

1H-Pyrazolo[4,3-c]pyridine-3,6(2H,5H)-dione, 2-(2-chlorophenyl)-4-[3-(dimethylamino)phenyl]-5-methyl-

References

1. Jiang JX, et al. Free Radic Biol Med. 2012 Jul 15;53(2):289-96.

2. Aoyama T, et al. Hepatology. 2012 Dec;56(6):2316-27.

3. Gray SP, et al. Circulation. 2013 May 7;127(18):1888-902.

4. Laleu B, et al. J Med Chem. 2010 Nov 11;53(21):7715-30.

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