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    Saxagliptin
    Saxagliptin

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0744
    CAS #: 361442-04-8 Purity ≥98%

    Description: Saxagliptin (also known as BMS-477118; brand name: Onglyza)  is a potent, orally bioactive, selective and reversible DPP4 (dipeptidyl peptidase-4) inhibitor with IC50 of 26 nM. Saxagliptin was approved in 2008 by FDA for the treatment of type 2 diabetes. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. In vitro, saxagliptin inhibits FBS-, insulin- and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin has no effect on ERK activation or cell proliferation.

    References: Adv Ther. 2009 Mar;26(3):249-62; J Med Chem. 2005 Jul 28;48(15):5025-37.

    Related CAS: 945667-22-1 (hydrate); 709031-78-7 (HCl); 1073057-20-1 (HCl hydrate); 1073057-33-6 (benzoate hydrate)  

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    Molecular Weight (MW)315.41
    FormulaC18H25N3O2
    CAS No.361442-04-8 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 63 mg/mL (199.7 mM)
    Water: 2 mg/mL (5.89 mM) 
    Ethanol: 24 mg/mL (76.1 mM)
    Solubility (In vivo)Saline: 30 mg/mL
    SynonymsBMS-477118; BMS477118; BMS 477118; brand name: Onglyza. 

    Chemical Name: (1S,3S,5S)-2-((S)-2-amino-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile

    SMILES Code: N#C[C@@H]1C[C@]2([H])[C@](C2)([H])N1C([C@H]([C@@]34C[C@@H]5C[C@H](C4)C[C@](C5)(O)C3)N)=O          


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: Saxagliptin H2O(BMS477118 H2O) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM. 


    Cell Assay: 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

    In VivoMaximal 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.
    Animal modelMale 13−14 week-old ob/ob mice
    Formulation & DosageDissolved in water; 10 μmol/kg; p.o. administration
    ReferencesAdv Ther. 2009 Mar;26(3):249-62; J Med Chem. 2005 Jul 28;48(15):5025-37.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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