955272-06-7
Chemical Structure
GKT136901
- CAS No.: 955272-06-7
- Formula:C19H15ClN4O2
- Molecular Weight:366.80
IUPAC Name: 2-(2-chlorophenyl)-4-methyl-5-(pyridin-2-ylmethyl)-1,2-dihydro-3H-pyrazolo[4,3-c]pyridine-3,6(5H)-dione
InChIKey: DNKYHHFCPXKFIY-UHFFFAOYSA-N
SMILES: O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O
Biological Activity: GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity[1][2][3].
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GKT136901 | 99.33% | GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity. | ||||||||||||||||||||
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GKT136901 (Standard) | ≥98% | GKT136901 (Standard) is the analytical standard of GKT136901. This product is intended for research and analytical applications. GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 is also a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity. | ||||||||||||||||||||
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References
- [1]. Laleu B, et, al. First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem. 2010 Nov 11;53(21):7715-30. [Content Brief]
- [2]. Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669. [Content Brief]
- [3]. Schildknecht S, et, al. The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr Med Chem. 2014;21(3):365-76. [Content Brief]
