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Setanaxib
Cat. No. IC23041
CAS. No. 1218942-37-0
Key Features and Details
Category
Inhibitor&Activator
Purity
99.45%
Formula
C21H19ClN4O2
Product Details
Product Name
Setanaxib
CAS No.
1218942-37-0
Molecular Weight
394.85
Synonyms
GKT137831; GKT831
Formula
C21H19ClN4O2
Appearance
Solid
Purity
99.45%
SMILES
O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C3=CC=CC(N(C)C)=C3)N4C)=CC4=O
Product Overview
Description
Setanaxib (GKT137831) is a selective NADPH oxidase (NOX1/4) inhibitor with Kis of 140 and 110 nM, respectively.
In Vitro Activity
Setanaxib (GKT137831) is a potent Nox1/4 inhibitor (Kis=140±40/110±30 nM). Administration of Setanaxib (GKT137831) throughout the 72-hour period of normoxia or hypoxia exposure attenuates HPASMC proliferation under normoxic conditions at the 20 μM concentration but had no effect on proliferation in normoxic HPAECs. In the prevention paradigm, Setanaxib (GKT137831) attenuates hypoxia-induced HPASMC and HPAEC proliferation at 5 and 20 μM. Complementary assays of cell proliferation measuring the expression of PCNA or manual cell counting confirmed that Setanaxib (GKT137831) attenuates hypoxia-induced pulmonary vascular cell proliferation.
In Vivo Activity
During the last half of CCl4 injections, some mice are treated with Setanaxib (GKT137831) daily. CCl4-induced liver fibrosis is more pronounced in SOD1mu compared to WT mice. Liver fibrosis in both SOD1mu and WT mice is attenuated by Setanaxib (GKT137831) treatment. The increased hepatic α-SMA expression is markedly decreased in SOD1mu mice treated with Setanaxib (GKT137831), to a level similar to that of WT mice given the NOX1/4 inhibitor.
Storage & Handling
Storage
Powder, -20 °C, 3 years; 4 °C, 2 years
In solvent: -80 °C, 6 months, -20 °C, 1 month.
Shipping
Room temperature in continental US; may vary elsewhere.
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