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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 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|
Tofogliflozin (CSG-452) hydrate is a potent and highly specific sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 value of 2.9 nM.
Luseogliflozin is a SGLT2 inhibitor, it reduced reabsorption of renal filtered glucose and decreased renal glucose threshold (RTG) in urine to increase urinary glucose excretion.
LX2761 is a locally acting SGLT1 and SGLT2 inhibitor in vitro with IC50 values of 2.2 nM and 2.7 nM for hSGLT1 and hSGLT2, respectively.
|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.
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