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.
Product information
CAS Number: 1254507-01-1
Molecular Weight: 407.29
Formula: C19H20Cl2N4O2
Chemical Name: 2-(2-chlorophenyl)-4-methyl-5-[(pyridin-2-yl)methyl]-octahydro-1H-pyrazolo[4,3-c]pyridine-3,6-dione hydrochloride
Smiles: Cl.CC1C2C(CC(=O)N1CC1=CC=CC=N1)NN(C1=CC=CC=C1Cl)C2=O
InChiKey: ZDPBRBFSARFUJA-UHFFFAOYSA-N
InChi: InChI=1S/C19H19ClN4O2.ClH/c1-12-18-15(10-17(25)23(12)11-13-6-4-5-9-21-13)22-24(19(18)26)16-8-3-2-7-14(16)20;/h2-9,12,15,18,22H,10-11H2,1H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (154.99 mM; Need ultrasonic). H2O : 4 mg/mL (9.92 mM; ultrasonic and warming and heat to 60°C).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GKT136901 (10 μM; 30 min) significantly attenuates high-D-glucose-induced increase in O2•− production and in H2O2 generation in MPT cells. GKT136901 (10 μM; 30 min) abolishes the effect of high D-glucose on p38MAP kinase activation in MPT cells. GKT136901 (10 μM; 2 h) attenuates methamphetamine (METH)-induced oxidative stress in HBMECs. GKT136901 (10 μM; 2 h) protects HBMECs against METH-induced blood-brain barrier (BBB) dysfunction.
In Vivo:
GKT136901 (30-90 mg/kg; daily p.o. for 16 weeks) has renoprotective effects in a mouse model of Type 2 diabetes.
Products are for research use only. Not for human use.
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