| Name | Canagliflozin hemihydrate |
| Description | Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories. |
| In vitro | Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4±1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684±159 nM and >1,000 nM, respectively[1]. |
| In vivo | Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice, while Canagliflozin (3 mg/kg for 3 weeks) increased urinary glucose excretion (UGE) without significant change in total food intake, resulting in decreased body weight in ZF rats[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 255 mg/mL (281.13 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (3.64 mM), Sonication is recommended.
|
| Keywords | SGLT2 | Canagliflozin Hemihydrate | Canagliflozin |
| Inhibitors Related | Dapagliflozin ((2S)-1,2-propanediol, hydrate) | Ertugliflozin L-pyroglutamic acid | Dapagliflozin | Sotagliflozin | Ipragliflozin | Mizagliflozin | Tofogliflozin (hydrate) | Phlorizin | Phloretin | Sergliflozin A | Empagliflozin | Canagliflozin |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
