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JNJ-28431754 (Canagliflozin) | SGLT2 inhibitor

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Price:
$149.00
Catalog #:
C2262-2s
Quantity:


Product Description

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.

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