Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2) for CHO-hSGLT2, CHO-rSGLT2 and CHO-mSGLT2 with IC50 of 4.4 nM, 3.7 nM and 2 nM, which is responsible for at least 90% of the glucose reabsorption in the kidney. Canagliflozin increased LDL cholesterol, urinary tract infections, genital mycotic infections, and was associated increased urination and episodes of hypotension and hypoglycemia. Canagliflozin shows pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice. Oral administration at 30 mg/kg of Canagliflozin to male SD rats induces glucose excretion over 24 hours by 3,696 mg per 200 g body weight. Dose dependently, canagliflozin decreased calculated 24-h mean RT(G) with maximal reduction to approximately 60 mg/dl, and increased mean 24-h UGE. At doses >200 mg administered before breakfast, canagliflozin reduced postprandial PG and serum insulin excursions at that meal. Canagliflozin was generally well tolerated. Canagliflozin has entered in a Phase III clinical trial for the treatment of diabetes mellitus and type 2 renal insufficiency.
|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.
|Solubility||DMSO 80 mg/mL|
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.
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.
Sha S, et al. Diabetes Obes Metab. 2011 Jul;13(7):669-72. PMID: 21457428.
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.
Nomura S, et al. J Med Chem. 2010 Sep 9;53(17):6355-60. PMID: 20690635.
|Related SGLT Products|
Canagliflozin hemihydrate (JNJ-28431754; TA 7284) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM.
|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.
Phloretin is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes.
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.
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