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GKT137831

Cat. No. M4828
GKT137831 Structure
Synonym:

Setanaxib

Size Price Availability Quantity
10mM*1mL USD 86.4  USD96 In stock
2mg USD 64.8  USD72 In stock
5mg USD 96.3  USD107 In stock
10mg USD 159.3  USD177 In stock
50mg USD 513  USD570 In stock
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Quality Control
Biological Activity

GKT137831 attenuated hypoxia-induced H(2)O(2) release, proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs in vitro. In vivo GKT137831 inhibited hypoxia-induced increases in TGF-β1 and reductions in PPARγ expression and attenuated RVH and pulmonary artery wall thickness but not increases in RVSP or muscularization of small arterioles.Targeting Nox4 with GKT137831 provides a novel strategy to attenuate hypoxia-induced alterations in pulmonary vascular wall cells that contribute to vascular remodeling and RVH, key features involved in PH pathogenesis.GKT137831, attenuated liver fibrosis and ROS production in both SOD1mu and WT mice as well as messenger RNA expression of fibrotic and NOX genes.Treatment with GKT137831 suppressed ROS production and NOX and fibrotic gene expression, but not Rac1 activity, in SOD1mut and WT HSCs. Both Ang II and tumor growth factor beta up-regulated NOX4, but Ang II required NOX1.GKT137831 is a potent inhibitor of fibrosis and hepatocyte apoptosis; therefore, it is a promising therapeutic agent for future translational studies.

Product Citations
Customer Product Validations & Biological Datas
Source Cell Physiol Biochem (2018). Figure 5. GKT137831
Method DCF assays
Cell Lines AML12 cells
Concentrations 0.2, 1 and 5 μM
Incubation Time 1 h
Results Importantly, the application of GKT137381 dose-dependently decreased the percentage of PA-induced apoptosis in cultured AML12 cells
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 394.85
Formula C21H19ClN4O2
CAS Number 1218942-37-0
Purity 99.01%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation.
Green DE, et al. Am J Respir Cell Mol Biol. 2012 Nov;47(5):718-26. PMID: 22904198.

Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent.
Aoyama T, et al. Hepatology. 2012 Dec;56(6):2316-27. PMID: 22806357.

Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo.
Jiang JX, et al. Free Radic Biol Med. 2012 Jul 15;53(2):289-96. PMID: 22618020.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GKT137831, Setanaxib supplier, inhibitors

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