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Saxagliptin (BMS-477118)

Name: Saxagliptin (BMS-477118)
Brand: Selleck Chemicals
SKU: S1540
Rating: 5 (5 reviews)

Catalog No.S1540 Synonyms: Onglyza

For research use only.

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

Saxagliptin (BMS-477118) Chemical Structure

CAS No. 361442-04-8

Selleck's Saxagliptin (BMS-477118) has been cited by 5 Publications

1 Customer Review

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DPP Signaling Pathway Map

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

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 K_i 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	MmrYSpVv[3Srb36gZZN{[Xl?				Mnq1TY5pcWKrdHnvckBw\iCqdX3hckBFWFB2IHX4dJJme3OnZDDpckBE[WOxLUKgZ4VtdHNuIFvpQVAvPiCwTR?=	NVvaW5pXOTdyM{SxOFg>

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In vivo

Maximal responses of Saxagliptin in glucose excursion in Zucker^fa/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 (from reference)

Animal Research:^[4]	Animal Models: Male 13−14 week-old ob/ob mice Dosages: 10 μmol/kg Administration: Orally

References

[4] Augeri DJ, et al. J Med Chem. 2005, 48(15), 5025-5037.

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Solubility (25°C)

In vitro


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

Chemical Information

Molecular Weight	315.41
Formula	C₁₈H₂₅N₃O₂
CAS No.	361442-04-8
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04445714	Recruiting	Drug: dapagliflozin and saxagliptin	Type 2 Diabetes Mellitus	AstraZeneca	April 7 2021	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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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