| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H16Cl2N4O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GKT136901 hydrochloride is a potent, selective and orally active inhibitor of NADPH oxidase NOX1/4, with Ki values of 160 nM and 165 nM, respectively. It also acts as a selective, direct scavenger of peroxynitrite and has anti-inflammatory activity, and can be used to study diabetic nephropathy, stroke, and neurodegeneration[1][2][3]. It is supplied as a light yellow to light brown solid (C19H16Cl2N4O2, MW 403.26) at 99.59% purity.
Physical & Chemical Properties
| CAS Number | 1254507-01-1 |
|---|---|
| Molecular Formula | C19H16Cl2N4O2 |
| Molecular Weight | 403.26 g/mol |
| Purity | 99.59% |
| Appearance | Solid |
| Color | Light yellow to light brown |
| SMILES | O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O.[H]Cl |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 62.5 mg/mL (154.99 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 4 mg/mL (9.92 mM; Requires sonication and warming and heat to 60°C) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
Ki: 160 (NOX1), 165 (NOX4)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 62.5 mg/mL (154.99 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 4 mg/mL (9.92 mM) | requires sonication and warming and heat to 60°C |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.16 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (5.16 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
In MPT cells, GKT136901 (10 μM; 30 min) significantly attenuates the high-D-glucose-induced increase in O2•− production and H2O2 generation[4]. GKT136901 (10 μM; 30 min) also eliminates the effect of high D-glucose on activation of p38MAP kinase in MPT cells[4]. In HBMECs, GKT136901 (10 μM; 2 h) attenuates oxidative stress induced by methamphetamine (METH)[5]. GKT136901 (10 μM; 2 h) also protects HBMECs from METH-induced blood-brain barrier (BBB) dysfunction[5].
In Vivo
Renoprotective effects of GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) are seen in a mouse model of Type 2 diabetes[6].
| Animal Model | Male db/db and db/m mice (8 weeks)[6] |
|---|---|
| Dosage | 30, 90 mg/kg |
| Administration | Daily p.o. for 16 weeks |
| Result | Reduced albuminuria, thiobarbituric acid-reacting substances (TBARS) and renal ERK1/2 phosphorylation and preserved renal structure in diabetic mice. Had no effect on plasma glucose, BP (blood pressure), and body weight. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Appl Phys Rev. 2026 Jan 21.
DEAD-box helicase DDX24 is essential for endothelial mitochondrial function to maintain the blood-brain barrier. Cell Rep 2025 Oct 15;44(10):116428. PMID: 41105514
Aβ40 Improves Cerebrovascular Endothelial Function via NOX4-Dependent Hydrogen Peroxide Release. Int J Mol Sci 2025 Jul 15;26(14):6759. PMID: 40725005
Metformin Attenuates TGF-β1-Induced Fibrosis in Salivary Gland: A Preliminary Study. Int J Mol Sci 2023 Nov 13;24(22):16260. PMID: 38003450
bioRxiv. 2026 Jul 1.
