Saxagliptin

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

For research use only.

Catalog No.S1540 Synonyms: BMS-477118

5 publications

CAS No. 361442-04-8

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

Selleck's Saxagliptin has been cited by 5 publications

Cancer Cell, 2018, 34(4):659-673

PubMed: 30270124 ( click the link to review the publication )

Turk J Pharm Sci, 2019, 16(2):227-233

PubMed: 32454718 ( click the link to review the publication )

J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1083:249-257

PubMed: 29554521 ( click the link to review the publication )

J Chromatogr B Analyt Technol Biomed Life Sci, 2018, 1081-1082:109-117

PubMed: 29518719 ( click the link to review the publication )

FEMS Microbiol Lett, 2016, 363(9)

PubMed: 27010012 ( click the link to review the publication )

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.

Purity & Quality Control

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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 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	NWXjU\|hCTnWwY4Tpc44h[XO\|YYm=				MVLJcohq[mm2aX;uJI9nKGi3bXHuJGRRWDRiZYjwdoV{e2WmIHnuJGNi[29vMjDj[YxteyxiS3m9NE43KG6P	NHPkVpYyPzB\|NEG0PC=>

... Click to View More Cell Line Experimental Data

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

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

References

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

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Solubility (25°C)

In vitro	DMSO	63 mg/mL (199.74 mM)
	Water	63 mg/mL (199.74 mM)
	Ethanol	24 mg/mL (76.09 mM)
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 Download Saxagliptin SDF

Molecular Weight	315.41
Formula	C₁₈H₂₅N₃O₂
CAS No.	361442-04-8
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	BMS-477118
Smiles	C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N

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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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

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

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Saxagliptin