Indoxyl sulfate is a metabolite of tryptophan, showing adverse effects on bones and the central nervous system, having been most frequently implicated as a contributor to renal disease progression and vascular disease
Indoxyl Sulfate-D5 potassium salt is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole,an intermediate generated from tryptophan by intestinal bacteria,by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A1*2)in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR)in HepG2 40/6 hepatoma cells (EC50 = 12.1 nM in a reporter assay). It also inhibits the organic anion transporter (OAT) isoforms OAT1 and OAT3 (Kis = 34.2 and 74.4 µM,respectively for the rat transporters)in S2 proximal tubule cells. Indoxyl sulfate (0.2 and 1 mM)increases superoxide anion and nitric oxide levels in isolated human mononuclear blood cells. It increases serum creatinine and blood urea nitrogen (BUN)levels in the 5/6 nephrectomized rat model of chronic renal failure when administered at a dose of 50 mg/kg.
AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.