Item no. |
HY-101499A-10mg |
Manufacturer |
MedChem Express
|
CASRN |
1254507-01-1 |
Amount |
10 mg |
Quantity options |
100 mg
10mM/1mL
10 mg
25 mg
50 mg
5 mg
|
Category |
|
Type |
Biochemicals |
Specific against |
other |
Purity |
99.90 |
Formula |
C19H16Cl2N4O2 |
Citations |
[1]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.<br>[2]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.<br>[3]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.<br>[4]Teixeira G, et, al. Therapeutic potential of NADPH oxidase 1/4 inhibitors. Br J Pharmacol. 2017 Jun;174(12):1647-1669.<br>[5]Schildknecht S, et, al. The NOX1/4 inhibitor GKT136901 as selective and direct scavenger of peroxynitrite. Curr Med Chem. 2014;21(3):365-76.<br>[6]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. |
Smiles |
O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O.[H]Cl |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Available |
|
Product Description |
GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 hydrochloride is also a selective and direct scavenger of peroxynitrite. GKT136901 hydrochloride can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 hydrochloride also has anti-inflammatory activity[1][2][3]. |
StorageTemperature |
4°C (Powder, sealed storage, away from moisture) |
Shipping |
Room Temperature |
Manufacturers Applications |
Metabolism-sugar/lipid metabolism |
MolecularWeight |
403.26 |
Clinical_Information |
No Development Reported |
Manufacturers Research Area |
Metabolic Disease; Neurological Disease |
Solubility |
DMSO : 62.5 mg/mL (ultrasonic)|H2O : 4 mg/mL (ultrasonic; warming; heat to 60°C) |
Manufacturers Target |
NADPH Oxidase |
Isoform |
NOX1; NOX4 |
Pathway |
Metabolic Enzyme/Protease |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.