GKT137831
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MedKoo CAT#: 522357

CAS#: 1218942-37-0

Description: GKT137831, also known as GTK831, is a novel and potent Nox4 inhibitor. GKT137831 reduced the increased leukocyte adherence to the vasculature, the pro-inflammatory phenotype of microglia and macroglia, the increased gene and protein expression of vascular endothelial growth factor, monocyte chemoattractant protein-1, and leukocyte adhesion molecules as well as vascular leakage. In all cultured cell types, GKT137831 reduced the hypoxia-induced increase in ROS levels and protein expression of various inflammatory mediators. GKT137831 may be potentially useful as a treatment for a variety of vision-threatening retinopathies.


Chemical Structure

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GKT137831
CAS# 1218942-37-0

Theoretical Analysis

MedKoo Cat#: 522357
Name: GKT137831
CAS#: 1218942-37-0
Chemical Formula: C21H19ClN4O2
Exact Mass: 394.11965
Molecular Weight: 394.85
Elemental Analysis: C, 63.88; H, 4.85; Cl, 8.98; N, 14.19; O, 8.10

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same day
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1650.0 Same day
1.0g USD 2950.0 2 Weeks
2.0g USD 4950.0 2 weeks
5.0g USD 8750.0 2 weeks
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Synonym: GKT137831; GKT-137831; GKT 137831; GTK831; GTK-831; GTK 831.

IUPAC/Chemical Name: 2-(2-chlorophenyl)-4-(3-(dimethylamino)phenyl)-5-methyl-1,2-dihydro-3H-pyrazolo[4,3-c]pyridine-3,6(5H)-dione

InChi Key: RGYQPQARIQKJKH-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H19ClN4O2/c1-24(2)14-8-6-7-13(11-14)20-19-16(12-18(27)25(20)3)23-26(21(19)28)17-10-5-4-9-15(17)22/h4-12,23H,1-3H3

SMILES Code: CN(C)C1=CC(C2=C(C(N(C3=CC=CC=C3Cl)N4)=O)C4=CC(N2C)=O)=CC=C1

Appearance: light yellow to yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 394.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Deliyanti D, Wilkinson-Berka JL. Inhibition of NOX1/4 with GKT137831: a potential novel treatment to attenuate neuroglial cell inflammation in the retina. J Neuroinflammation. 2015 Jul 30;12:136. doi: 10.1186/s12974-015-0363-z. PubMed PMID: 26219952; PubMed Central PMCID: PMC4518508.

2: Green DE, Murphy TC, Kang BY, Kleinhenz JM, Szyndralewiez C, Page P, Sutliff RL, Hart CM. The Nox4 inhibitor GKT137831 attenuates hypoxia-induced pulmonary vascular cell proliferation. Am J Respir Cell Mol Biol. 2012 Nov;47(5):718-26. doi: 10.1165/rcmb.2011-0418OC. Epub 2012 Aug 16. PubMed PMID: 22904198; PubMed Central PMCID: PMC3547100.

3: Aoyama T, Paik YH, Watanabe S, Laleu B, Gaggini F, Fioraso-Cartier L, Molango S, Heitz F, Merlot C, Szyndralewiez C, Page P, Brenner DA. Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology. 2012 Dec;56(6):2316-27. doi: 10.1002/hep.25938. PubMed PMID: 22806357; PubMed Central PMCID: PMC3493679.

4: Jiang JX, Chen X, Serizawa N, Szyndralewiez C, Page P, Schröder K, Brandes RP, Devaraj S, Török NJ. Liver fibrosis and hepatocyte apoptosis are attenuated by GKT137831, a novel NOX4/NOX1 inhibitor in vivo. Free Radic Biol Med. 2012 Jul 15;53(2):289-96. doi: 10.1016/j.freeradbiomed.2012.05.007. Epub 2012 May 19. PubMed PMID: 22618020; PubMed Central PMCID: PMC3392471.