Canagliflozin
SGLT2 inhibitor / Potent inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), IC50 = 2.2 nM selective over SGLT1, IC50=910 nM.1 Dose dependently increases glucose excretion in healthy subjects.2 Displays beneficial effects in nonalcoholic fatty liver disease (NAFLD).3 Extends lifespan in male but not female mice.4 Inhibits cancer cell proliferation via inhibition of mitochondrial complex-1 supported respiration.5 Suppresses the growth of pancreatic cancer cells.6
Biochemicals & reagents
842133-18-0
JNJ-24831754
1) Nomura et al. (2010), Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus; J. Med. Chem., 53 6355 2) Shaw et al. (2011), Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects; Diabetes Obes. Metab., 13 669 3) Mantovani et al. (2020), Sodium-Glucose Cotransporter-2 Inhibitors for Treatment of Nonalcoholic Fatty Liver Disease: A Meta-Analysis of Randomized Controlled Trials; Metabolites, 11 22 4) Miller et al. (2020), Canagliflozin extends life span in genetically heterogeneous male but not female mice; JCI Insight, 5 e140019 5) Vilani et al. (2016), The diabetes medication Canagliflozin reduces cancer cell proliferation by inhibiting mitochondrial complex-I supported respiration; Mol. Metab., 5 1048 6) Xu et al. (2020), Inhibitory effects of canagliflozin on pancreatic cancer are mediated via the downregulation of glucose transporter-1 and lactate dehydrogenase A; Int. J, Oncol., Sept. 8 (online ahead of print)
-20°C
TARGET: Glucose transporter -- PATHWAY: Carbohydrate metabolism; Proliferation; Mitochondrial function; Senescence -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer; DiabetesHypertension; Ageing; Liver disease