1062624-71-8
Chemical Structure
GK-136901
- CAS No.: 1062624-71-8
- Formula:C20H18N4O2
- Molecular Weight:346.38
IUPAC Name: 4-methyl-5-(pyridin-2-ylmethyl)-2-(o-tolyl)-1,2-dihydro-3H-pyrazolo[4,3-c]pyridine-3,6(5H)-dione
InChIKey: FJPUXMVNLPHRCZ-UHFFFAOYSA-N
SMILES: O=C1C=C2NN(C3=C(C)C=CC=C3)C(C2=C(C)N1CC4=NC=CC=C4)=O
Biological Activity: 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[1][2][3][4].
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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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- [1]. Weaver J R, Grzesik W, Taylor-Fishwick D A. Inhibition of NADPH oxidase-1 preserves beta cell function[J]. Diabetologia, 2015, 58(1): 113-121.
- [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]
- [3]. Sedeek M, et al. Critical role of Nox4-based NADPH oxidase in glucose-induced oxidative stress in the kidney: implications in type 2 diabetic nephropathy[J]. American Journal of Physiology-Renal Physiology, 2010, 299(6): F1348-F1358.
- [4]. Schramm A, et al. Targeting NADPH oxidases in vascular pharmacology. Vascul Pharmacol. 2012;56(5-6):216-231. [Content Brief]
Keywords
