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GKT136901 hydrochloride (Alias: GKT-901 hydrochloride, GKT-771 hydrochloride, GKT-136901 hydrochloride, AK...)

Name: GKT136901 hydrochloride
Brand: TargetMol
SKU: T38646
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T38646 Copy Product Info

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GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.

GKT136901 hydrochloride

Copy Product Info

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Catalog No. T38646

Alias GKT-901 hydrochloride, GKT-771 hydrochloride, GKT-136901 hydrochloride, AK120765 hydrochloride, AK 120765 hydrochloride

GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.

Cas No. 1254507-01-1

Pack Size	Price	USA Stock	Global Stock	Quantity
2 mg	$29	-	In Stock

In stock · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Appearance:Solid

Color:Yellow

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COA

Product Introduction

Bioactivity

Description	GKT136901 hydrochloride is a NOX-1/4 inhibitor, a selective scavenger of peroxynitrite, which inhibits METH-induced ROS production.
Targets&IC50	NOX1:160 nM (Ki), NOX4:165 nM (Ki)
In vitro	GKT136901 hydrochloride is a potent, selective and orally active NADPH oxidase (NOX1/4) inhibitor with Ki values of 160 nM and 165 nM, respectively. [1] GKT136901 hydrochloride significantly reduced the production of superoxide radical anion and H2O2 in MPT cells induced by high D-glucose and eliminated the effect of high D-glucose on p38MAP kinase activation in MPT cells after treatment with GKT136901 hydrochloride at a dose of 10 μM for 30 min. [3] GKT136901 hydrochloride attenuated methamphetamine (METH)-induced oxidative stress in HBMEC treated at a dose of 10 μM for 2 hours and effectively protected HBMEC from METH-induced blood-brain barrier (BBB) dysfunction. [5]
In vivo	GKT136901 hydrochloride exhibited nephroprotective effects in a mouse model of type 2 diabetes mellitus when administered orally at a dose of 30-90 mg/kg daily for 16 weeks. [6]
Synonyms	GKT-901 hydrochloride, GKT-771 hydrochloride, GKT-136901 hydrochloride, AK120765 hydrochloride, AK 120765 hydrochloride

Chemical Properties

Molecular Weight	403.26
Formula	C₁₉H₁₆Cl₂N₄O₂
Cas No.	1254507-01-1
Smiles	Cl.O=C1C=C2NN(C(=O)C2=C(N1CC3=NC=CC=C3)C)C=4C=CC=CC4Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 2 mg/mL (4.96 mM), Sonication is recommended.

DMSO: 50 mg/mL (123.99 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4798 mL	12.3989 mL	24.7979 mL	123.9895 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.4960 mL	2.4798 mL	4.9596 mL	24.7979 mL
10 mM	0.2480 mL	1.2399 mL	2.4798 mL	12.3989 mL
20 mM	0.1240 mL	0.6199 mL	1.2399 mL	6.1995 mL
50 mM	0.0496 mL	0.2480 mL	0.4960 mL	2.4798 mL
100 mM	0.0248 mL	0.1240 mL	0.2480 mL	1.2399 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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