Saxagliptin is an orally-available, adamantyl-based, reversible inhibitor of DPP-IV for the treatment of Type 2 diabetes with an IC50 of 26 nM and Ki of 0.6-1.3 nM [1, 2]. Saxagliptin is more selective than other approved DPP-IV inhibitors (vildagliptin, sitagliptin) and is 400-fold and 75-fold selective over DPP-VIII and DPP-IX, respectively. [1] Once-daily administration of saxagliptin either as a monotherapy or in combination results in a significant reductions in fasting and postprandial plasma glucose and HbA1c.
Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, improving b-cell function and suppression of glucagon secretion. [2]
Technical information:
Chemical Formula: | C18H25N3O2 | |
CAS #: | 361442-04-8 | |
Molecular Weight: | 315.41 | |
Purity: | >98% | |
Appearance: | White | |
Chemical Name: | (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl) acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile | |
Solubility: | Up to 22 mM in DMSO | |
Synonyms: | BMS-477118, BMS 477118, BMS477118, Saxagliptin, Onglyza |
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. | Tahrani et al., Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus. Adv. Ther. 2009, 26(3), 249-262. Pubmed ID: 19330494 |
2. | Deacon et al., Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Adv. Ther. 2009, 26(5), 488-499. Pubmed ID: 19444391 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.