Catalog No.S1540 Synonyms: BMS-477118
Molecular Weight(MW): 315.41
Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Purity & Quality Control
Choose Selective DPP-4 Inhibitors
|Description||Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.|
Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9).  Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion. 
|In vivo||Maximal responses of Saxagliptin in glucose excursion in Zuckerfa/fa rats are associated with plasma DPP4 inhibition of approximately 60% vs. control, and no additional antihyperglycemic effects are seen at higher percent inhibition. Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT. |
|In vitro||DMSO||63 mg/mL (199.74 mM)|
|Water||63 mg/mL (199.74 mM)|
|Ethanol||24 mg/mL (76.09 mM)|
|In vivo||Add solvents to the product individually and in order:
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02917031||Recruiting||Type 2 Diabetes Mellitus|Heart Failure||AstraZeneca||January 2017||Phase 4|
|NCT02377388||Not yet recruiting||Platelet Aggregation During Acute Myocardial Infarction||University of Sao Paulo General Hospital|InCor Heart Institute||December 2016||Phase 3|
|NCT02965443||Not yet recruiting||Type 2 Diabetes||University Hospital Tuebingen||December 2016||Phase 4|
|NCT02765204||Completed||Diabetes Mellitus, Type 2||Uppsala University|AstraZeneca||March 2016||Phase 4|
|NCT02681094||Active, not recruiting||Type2 Diabetes Mellitus|Inadequate Glycaemic Control||AstraZeneca||February 2016||Phase 3|
|NCT02613897||Recruiting||Diabetes Mellitus, Type 2||The University of Texas Health Science Center at San Antonio|AstraZeneca||January 2016||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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