Saxagliptin

Catalog No.S1540 Synonyms: BMS-477118

Saxagliptin Chemical Structure

Molecular Weight(MW): 315.41

Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

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Biological Activity

Description Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Targets
DPP-4 [1]
26 nM
In vitro

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). [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Caco-2 cells M3XlOWZ2dmO2aX;uJIF{e2G7 NWDMdHVyUW6qaXLpeIlwdiCxZjDoeY1idiCGUGC0JIV5eHKnc4Pl[EBqdiCFYXPvMVIh[2WubIOsJGtqRTBwNjDuUS=> MYWxO|A{PDF2OB?=

... Click to View More Cell Line Experimental Data

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. [4]

Protocol

Animal Research:[4]
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  • Animal Models: Male 13−14 week-old ob/ob mice
  • Formulation: Water
  • Dosages: 10 μmol/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

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:
Saline
30 mg/mL

* 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.

Chemical Information

Molecular Weight 315.41
Formula

C18H25N3O2

CAS No. 361442-04-8
Storage powder
Synonyms BMS-477118

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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 --

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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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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID