Canagliflozin hemihydrate is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Canagliflozin hemihydrate inhibits hSGLT2 with IC50 of 2.2 nM, exhibits 413-fold selectivity over hSGLT1. Blocking SGLT2 causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Effect of canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, on bacteriuria and urinary tract infection in subjects with type 2 diabetes enrolled in a 12-week, phase 2 study.
Nicolle LE, et al. Curr Med Res Opin. 2012 Jul;28(7):1167-71. PMID: 22548646.
Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes.
Rosenstock J, et al. Diabetes Care. 2012 Jun;35(6):1232-8. PMID: 22492586.
Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models.
Liang Y, et al. PLoS One. 2012;7(2):e30555. PMID: 22355316.
|Related SGLT Products|
|Dapagliflozin ((2S)-1,2-propanediol, hydrate)
Dapagliflozin(BMS512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2) is in development for the treatment of type 2 diabetes mellitus (T2DM).
LX-4211 is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively.
Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6.
Canagliflozin is a potent, selective sodium glucose co-transporter 2 inhibitor.
Dapagliflozin is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2).
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