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GKT136901 hydrochloride

Catalog No. T38646 CAS 1254507-01-1

Synonyms: GKT136901 hydrochloride

GKT136901 hydrochloride is a powerful, selective, and orally active inhibitor of NADPH oxidase (NOX1/4). It exhibits K i values of 160 nM and 165 nM against NOX1 and NOX4, respectively. Additionally, GKT136901 hydrochloride demonstrates selectivity and direct scavenging ability towards peroxynitrite. This compound finds utility in studying diabetic nephropathy, stroke, neurodegeneration, and possesses anti-inflammatory properties.

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GKT136901 hydrochloride Chemical Structure

GKT136901 hydrochloride, CAS 1254507-01-1

Pack Size	Availability	Price/USD
5 mg	5 days	$ 39.00
10 mg	5 days	$ 73.00
1 mL * 10 mM (in DMSO)	5 days	$ 45.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	GKT136901 hydrochloride is a powerful, selective, and orally active inhibitor of NADPH oxidase (NOX1/4). It exhibits K i values of 160 nM and 165 nM against NOX1 and NOX4, respectively. Additionally, GKT136901 hydrochloride demonstrates selectivity and direct scavenging ability towards peroxynitrite. This compound finds utility in studying diabetic nephropathy, stroke, neurodegeneration, and possesses anti-inflammatory properties.
In vitro	GKT136901 (10 μM; 30 min) effectively reduces the increase in O2?? production and H2O2 generation in MPT cells caused by high-D-glucose[4]. It also eliminates high D-glucose's effect on p38MAP kinase activation in MPT cells[4]. Additionally, when applied for 2 hours, GKT136901 (10 μM) mitigates methamphetamine (METH)-induced oxidative stress and protects against METH-induced blood-brain barrier (BBB) dysfunction in HBMECs[5].
In vivo	GKT136901, administered orally at doses of 30-90 mg/kg daily for 16 weeks, exhibits renoprotective effects in a male db/db and db/m mouse model of Type 2 diabetes. This regimen notably reduces albuminuria, thiobarbituric acid-reacting substances (TBARS), and renal ERK1/2 phosphorylation, while preserving the renal structure in diabetic mice. It does not, however, affect plasma glucose levels, blood pressure (BP), or body weight.

Synonyms	GKT136901 hydrochloride
Molecular Weight	403.26
Formula	C19H16Cl2N4O2
CAS No.	1254507-01-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 2. Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669. 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. 4. 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. Am J Physiol Renal Physiol. 2010 Dec;299(6):F1348-58. 5. Hwang JS, et, al. GKT136901 protects primary human brain microvascular endothelial cells against methamphetamine-induced blood-brain barrier dysfunction. Life Sci. 2020 Sep 1;256:117917. 6. Sedeek M, et, al. Renoprotective effects of a novel Nox1/4 inhibitor in a mouse model of Type 2 diabetes. Clin Sci (Lond). 2013 Feb;124(3):191-202.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GKT136901 hydrochloride 1254507-01-1 GKT-136901 Hydrochloride GKT136901 Hydrochloride GKT-136901 hydrochloride GKT 136901 Hydrochloride inhibitor inhibit

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