[CAS NO. 1218942-37-0] Setanaxib (GKT137831)

Name: Setanaxib (GKT137831)
Brand: Arctom Scientific
SKU: SLK-S7171

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PRODUCTS SPECIFICATIONS [1218942-37-0]

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Catalog

SLK-S7171

Brand

Selleck

CAS

1218942-37-0

DESCRIPTION [1218942-37-0]

Overview

MDL	MFCD27923122
Molecular Weight	394.85
Molecular Formula	C21H19ClN4O2
SMILES	O=C1C2=C(N(C)C(=O)C=C2NN1C3=C(Cl)C=CC=C3)C4=CC(N(C)C)=CC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.5326 mL	12.6630 mL	25.3261 mL
5 mM	0.5065 mL	2.5326 mL	5.0652 mL
10 mM	0.2533 mL	1.2663 mL	2.5326 mL
50 mM	0.0507 mL	0.2533 mL	0.5065 mL

Description

Setanaxib (GKT137831, GKT831) is a potent, dual inhibitor with of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses production. GKT137831 partly inhibits .

Targets

Ferroptosis ^[5]	NOX1 ^[1] (Cell-based assay)	NOX4 ^[1] (Cell-based assay)
	110 nM(Ki)	140 nM(Ki)

In vitro

GKT137831 attenuates hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs. GKT137831 also prevents oxidative stress in response to hyperglycemia in human aortic endothelial cells.

References

[1] Aoyama T, et al. Hepatology. 2012, 56(6), 2316-2327.
[2] Green DE, et al. Am J Respir Cell Mol Biol. 2012, 47(5), 718-726.
[3] Gray SP, et al. Circulation. 2013, 127(18), 1888-1902.
[4] Zhao QD, et al. 2015, Doi:10.1161/CIRCULATIONAHA.114.011079.
[5] Jasmin Dächert, et al. Int J Cancer . 2020 Jan 15;146(2):510-520.

Synonyms

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

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

GKT 831

Setanaxib

GKT 137831

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