1. Metabolic Enzyme/Protease
  2. NADPH Oxidase
  3. GKT136901 hydrochloride

GKT136901 hydrochloride 

Cat. No.: HY-101499A
Handling Instructions

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.

For research use only. We do not sell to patients.

GKT136901 hydrochloride Chemical Structure

GKT136901 hydrochloride Chemical Structure

CAS No. : 1254507-01-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 75 In-stock
Estimated Time of Arrival: December 31
25 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 280 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target

Ki: 160 (NOX1), 165 (NOX4)[1]

In Vitro

GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O2•− production and in H2O2 generation in MPT cells[4].
GKT136901 (10 μM; 30 min) abolishes the effect of high D-glucose on p38MAP kinase activation in MPT cells[4].
GKT136901 (10 μM; 2 h) attenuates methamphetamine (METH)-induced oxidative stress in HBMECs[5].
GKT136901 (10 μM; 2 h) protects HBMECs against METH-induced blood-brain barrier (BBB) dysfunction[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

403.26

Formula

C₁₉H₁₆Cl₂N₄O₂

CAS No.
SMILES

O=C1N(C2=CC=CC=C2Cl)NC(C1=C(C)N3CC4=NC=CC=C4)=CC3=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (154.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4798 mL 12.3989 mL 24.7979 mL
5 mM 0.4960 mL 2.4798 mL 4.9596 mL
10 mM 0.2480 mL 1.2399 mL 2.4798 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.16 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.16 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GKT136901GKT 136901GKT-136901NADPH OxidaseNOXNADPHoxidaseNOX1/4scavengerperoxynitritediabeticnephropathystrokeneurodegenerationanti-inflammatoryInhibitorinhibitorinhibit

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Product Name:
GKT136901 hydrochloride
Cat. No.:
HY-101499A
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