GK-136901
GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a Ki of 160 nM for Nox1 and 165 nM for Nox4. GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin (fibronectin) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension.
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- CAS No.: 1062624-71-8
- Formule: C20H18N4O2
- Masse moléculaire:346.38
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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NOX4 165 nM (Ki) |
NOX1 160 nM (Ki) |
In Vitro
GKT136901 (10 μM; 30 min) inhibits NADPH oxidase activity and ROS production induced by high D-glucose in MPT cells[2].
GKT136901 (10 μM; 30 min) inhibits the expression of profibrotic proteins and the activation of p38MAP kinase in MPT cells induced by high D-glucose[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Immortalized mouse proximal tubule (MPT) cells
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Concentration:10 μM
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Incubation Time:30 min pre-incubation; 2 hr high D-glucose exposure
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Result:Abolished high D-glucose-induced phosphorylation of p38MAP kinase.
Showed no significant effect on p38MAP kinase phosphorylation when used alone or in combination with high L-glucose.
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Cell Line:Immortalized mouse proximal tubule (MPT) cells
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Concentration:10 μM
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Incubation Time:30 min pre-incubation; high D-glucose exposure
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Result:Inhibited high D-glucose-induced increases in TGF-β1/2 protein expression.
Inhibited high D-glucose-induced increases in fibronectin protein expression.
In Vivo
GK-136901 is well tolerated in mice, with oral administration doses tested up to 1000 mg/kg[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1062624-71-8
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Masse moléculaire 346.38
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Formule C20H18N4O2
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SMILES
O=C1C=C2NN(C3=C(C)C=CC=C3)C(C2=C(C)N1CC4=NC=CC=C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[2]. Harrison IP, et al. Understanding the biology of reactive oxygen species and their link to cancer: NADPH oxidases as novel pharmacological targets. Clin Exp Pharmacol Physiol. 2014;41(8):533-542. [Content Brief]
[4]. Schramm A, et al. Targeting NADPH oxidases in vascular pharmacology. Vascul Pharmacol. 2012;56(5-6):216-231. [Content Brief]
[5]. Rodiño-Janeiro BK, et al. Current status of NADPH oxidase research in cardiovascular pharmacology. Vasc Health Risk Manag. 2013;9:401-428. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GK-136901 Related Classifications
HY-124487 Related Classifications
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