Saxagliptin

For research use only.

Catalog No.S1540 Synonyms: BMS-477118

5 publications

Saxagliptin Chemical Structure

CAS No. 361442-04-8

Saxagliptin (Vadimezan, NSC 640488, ASA-404) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 412 In stock
EUR 314 In stock
EUR 658 In stock
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Selleck's Saxagliptin has been cited by 5 publications

1 Customer Review

  • Mean plasma concentration-time profiles of saxagliptin after oral administration of a test and a reference SPC formulation of saxagliptin/metformin XR tablet (5 mg/500 mg) to 10 healthy Chinese subjects. The inserted represented for the semi-log graph.

    J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1081-1082:109-117. Saxagliptin purchased from Selleck.

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Biological Activity

Description Saxagliptin (Vadimezan, NSC 640488, ASA-404) 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 M4ja[2Z2dmO2aX;uJIF{e2G7 M{HSdWlvcGmkaYTpc44hd2ZiaIXtZY4hTFCSNDDlfJBz\XO|ZXSgbY4hS2Glbz2yJINmdGy|LDDLbV0xNjZibl2= MnPmNVcxOzRzNEi=

... 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
  • 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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
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
in solvent
Synonyms BMS-477118
Smiles C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04445714 Not yet recruiting Drug: dapagliflozin and saxagliptin Type 2 Diabetes Mellitus AstraZeneca June 30 2020 Phase 4
NCT04521049 Completed Drug: Saxagliptin 5mg Diabetes Mellitus Type 2 Beni-Suef University March 1 2019 Phase 4
NCT02462369 Unknown status Drug: Saxagliptin|Drug: glimepiride Microalbuminuria|Microalbuminuria /Creatinine Ratios ACR The Second Hospital of Nanjing Medical University June 2015 Phase 4
NCT02280486 Completed Drug: Saxagliptin|Drug: Glimepiride Type 2 Diabetes The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School|The First Affiliated Hospital with Nanjing Medical University|Zhongda Hospital|Nanjing PLA General Hospital|Changzhou No.2 People''s Hospital|The First Affiliated Hospital of Soochow University|Wuxi People''s Hospital|The First Affiliated Hospital of Anhui Medical University|Huai''an First People''s Hospital January 2015 Phase 4

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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID