Canagliflozin is an orally-available, C-aryl glucoside inhibitor of hSGLT2, rSGLT2, and mSGLT2 cells at a potency of 4.4, 3.7, and 2.0 nM, respectively. [1] It inhibits AMG uptake in CHO-hSGLT1 cells with an IC50 of 684 nM. Canagliflozin lowers renal glucose resorptive capacity and increases urinary glucose excretion. Additionally, Canagliflozin has been shown to improve beta-cell function in ZDF rats, reduce body weight, increase fatty acid oxidation, and reduce de novo lipgenesisin rodent models of insulin resistance and Type II diabetes mellitus. [1]
In a twelve week study, Canagliflozin reduces HbA1c slightly more than sitagliptin (-0.21%) in a dose-dependent manner. [2] Reductions in blood pressure have also been observed in similar studies. Canagliflozin was approved by the FDA for the treatment of Type 2 diabetes in January, 2013.
Technical information:
| Chemical Formula: | C24H25FO5S | |
| CAS #: | 842133-18-0 | |
| Molecular Weight: | 444.52 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | JNJ-28431754 , JNJ 28431754, TA-7284, Canagliflozin, Invokana |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Liang et al., Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS ONE, 2012, 7(2), e30555. Pubmed ID: 22355316 |
| 2. | Clar et al., Systematic review of SGLT2 receptor inhibitors in dual or triple therapy in type 2 diabetes. BMJ Open, 2012, 2, e001007. Pubmed ID: 23087012 |
| 3. | Nomura et al., 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. J. Med. Chem. 2010, 53, 6355-6360. Pubmed ID: 20690635 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
