Setanaxib (GKT137831) - Moligand™, 10mM in DMSO , Inhibitor of cytochrome b-245 beta chain;Inhibitor of NADPH oxidase 1;Inhibitor of NADPH oxidase 4;Inhibitor of NADPH oxidase 5, CAS No.1218942-37-0, Inhibitor of cytochrome b-245 beta chain;Inhibitor of NADPH oxidase 1;Inhibitor of NADPH oxidase 4;Inhibitor of NADPH oxidase 5

CAS: 1218942-37-0 Cat. No.: S407890 Peso molecular: 394.85 Número EC: 942-974-8 PubChem CID: 58496428
Disponible para pedir
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
GKT831 | 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1,2-dihydro-5H-pyrazolo[4,3-c]pyridine-3,6-dione
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
 ·  off list, applied to all prices below.
Size
Estado
Price
Qty
1ml
S407890-1ml
1

216,90US$

315,90US$
Guardar 99,00 US$ (31.34%)
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 1 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Descripción general

Information

Setanaxib (GKT137831) Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits f
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.

In vivo

In WT and SOD1mut mice, GKT137831 (60 mg/kg i.g.) blocks liver fibrosis and downregulates markers of oxidative stress, inflammation, and fibrosis. GKT137831 (60 mg/kg/d p.o.) also attenuates chronic hypoxia–induced right ventricular hypertrophy, vascular remodeling, lung cell proliferation, and hypoxic alterations in lung PPARγ and TGF-β1 expression in mouse model of chronic hypoxia exposure. In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. Moreover, in angII-infused c-hNox4Tg mice, GKT137831 abolishes the increase in oxidative stress, suppresses Akt-mTOR and NF-κB signaling pathway and attenuates cardiac remodeling.
Cell Data

cell lines:

Concentrations:20 μM

Incubation Time:72 hours

Powder Purity:≥99%

Specifications

Sinónimos
GKT831 | 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1, 2-dihydro-5H-pyrazolo[4, 3-c]pyridine-3, 6-dione
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of cytochrome b-245 beta chain;Inhibitor of NADPH oxidase 1;Inhibitor of NADPH oxidase 4;Inhibitor of NADPH oxidase 5
Propiedades del producto
ALogP2.366
Recuento HBD1
Enlace rotable3
Nombres e identificadores
Isómeros SMILES CN1C(=O)C=C2C(=C1C3=CC(=CC=C3)N(C)C)C(=O)N(N2)C4=CC=CC=C4Cl
CAS alternativo 1218942-37-0
PubChem CID 58496428
Términos de entrada MeSH 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1H-pyrazolo(4,3-c)pyridine-3,6(2H,5H)-dione;GKT-137831;GKT-831;GKT137831;setanaxib
Peso molecular 394.85

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Objetivos asociados (humanos)
CYBB Tchem Cytochrome b-245 heavy chain (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NOX1 Tchem NADPH oxidase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NOX4 Tchem NADPH oxidase 4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NOX5 Tchem NADPH oxidase 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificados (CoA, COO, BSE/TSE y tabla de análisis)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propiedades químicas y físicas
DMSO (mg/ml) Solubilidad máxima78
DMSO (mM) Solubilidad máxima197.5433709
Agua (mg/ml) Solubilidad máxima<1
Citations of This Product
Referencias
1. Xiaoyong Huang, Qianqian Li, Shaobo Yun, Xiaomin Ren, Sijie Wu, Jia Cheng.  (2025)  Psoralea corylifolia seed extract bakuchiol hijacks bacterial metabolism to induce oxygen-dependent membrane lipid peroxidation in methicillin-resistant Staphylococcus aureus.  BIOORGANIC CHEMISTRY,      [PMID:41151326] [10.1016/j.bioorg.2025.109154]
Calculadoras de soluciones
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