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Saxagliptin (BMS-477118) DPP inhibitor

Name: Saxagliptin (BMS-477118)
SKU: S1540
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S1540

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

Chemical Structure

Molecular Weight: 315.41

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	315.41	Formula	C₁₈H₂₅N₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	361442-04-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Onglyza,BMS-477118			Smiles	C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (199.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 63 mg/mL

Ethanol : 63 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (95.11mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	DPP-4 ^[1] 26 nM
In vitro	Saxagliptin (BMS-477118) 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, it demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of this compound 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] It 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	Saxagliptin (BMS-477118) 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. Maximal responses of this compound 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. It dose-dependently elevates plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/19330494/ [2] https://pubmed.ncbi.nlm.nih.gov/19065993/ [3] https://pubmed.ncbi.nlm.nih.gov/19444391/ [4] https://pubmed.ncbi.nlm.nih.gov/16033281/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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