Home Proteases DPP inhibitor Saxagliptin (BMS-477118) For research use only.

Saxagliptin (BMS-477118)

Synonyms: Onglyza,BMS-477118

Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Saxagliptin (BMS-477118) Chemical Structure

Saxagliptin (BMS-477118) Chemical Structure

CAS No. 361442-04-8

Purity & Quality Control

Saxagliptin (BMS-477118) Related Products

Signaling Pathway

DPP Signaling Pathways

DPP Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Caco-2 cells Function assay Inhibition of human DPP4 expressed in Caco-2 cells, Ki=0.6 nM 17034148
Click to View More Cell Line Experimental Data

Biological Activity

Description Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Targets
DPP-4 [1]
26 nM
In vitro
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]
In Vivo
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]
Animal Research Animal Models Male 13−14 week-old ob/ob mice
Dosages 10 μmol/kg
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04445714 Completed
Type 2 Diabetes Mellitus
AstraZeneca
 April 7 2021 Phase 4
NCT04521049 Completed
Diabetes Mellitus Type 2
Beni-Suef University
 March 1 2019 Phase 4
NCT03199053 Completed
Diabetes Mellitus Type 2
AstraZeneca
 October 11 2017 Phase 3
NCT02462369 Unknown status
Microalbuminuria|Microalbuminuria /Creatinine Ratios ACR
The Second Hospital of Nanjing Medical University
 June 2015 Phase 4

Chemical Information & Solubility

Molecular Weight 315.41 Formula

C18H25N3O2
CAS No. 361442-04-8 SDF Download Saxagliptin (BMS-477118) SDF
Smiles C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 63 mg/mL

Ethanol : 63 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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