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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.
| Molecular Weight | 444.52 |
| Formula | C24H25FO5S |
| CAS Number | 842133-18-0 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related SGLT Products |
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| Dapagliflozin
Dapagliflozin (BMS-512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2). |
| Empagliflozin
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. |
| Phloridzin
Phloridzin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. |
| Phloretin
Phloretin (NSC 407292; RJC 02792) is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). |
| Sotagliflozin
Sotagliflozin (LX-4211) is an orally active, first-in-class dual SGLT1/2 inhibitor with IC50s of 36 nM and 1.8 nM, respectively, and is used in studies related to type 1 diabetes and heart failure. |
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