Home Proteases DPP inhibitor Saxagliptin hydrate For research use only.

Saxagliptin hydrate

Synonyms: BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate

Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Saxagliptin hydrate Chemical Structure

Saxagliptin hydrate Chemical Structure

CAS: 945667-22-1

Selleck's Saxagliptin hydrate has been cited by 1 publication

Purity & Quality Control

Batch: S469701 DMSO] 66 mg/mL] false] Ethanol] 66 mg/mL] false] Water] 1 mg/mL] false Purity: 99.54%
99.54

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Biological Activity

Description Saxagliptin H2O (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 In vitro, saxagliptin inhibits FBS-, insulin- and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin has no effect on ERK activation or cell proliferation. In both MSC and MC3T3E1 cells, saxagliptin in the presence of FBS inhibits Runx2 and osteocalcin expression, type-1 collagen production and mineralization, while increasing PPAR-gamma expression[4].
Cell Research Cell lines Marrow stromal cells(MSC); MC3T3E1 osteoblast-like cells
Concentrations 1.5 or 15 μM
Incubation Time 24 h or 1 h
Method

Sub-confluent cells are serum-starved overnight and then incubated with 1.5 or 15 μM saxagliptin and/or FBS (1%), insulin (5 ng/mL) or IGF1 (10-8 M) for 24 h (effects on cell proliferation) or 1 h (effects on signal transduction mechanisms).
In Vivo
In vivo Saxagliptin exerts direct beneficial effects on the arterial wall in an animal model of type 2 diabetes by increasing NO availability and improving antioxidant status. Saxagliptin reverses vascular hypertrophic remodeling and ameliorates NO availability in small arteries from db/db mice through the abrogation of NAD(P)H oxidase-driven eNOS uncoupling and by reducing the action of cyclooxygenase-1-derived vasoconstrictors downregulating the expression of thromboxane-prostanoid receptors[2]. DPP-4 inhibition with saxagliptin also improves pancreatic β-cell function in postprandial and fasting states, and decreases postprandial glucagon concentration[3].
Animal Research Animal Models adult mice C57BLKS/J; db/db mice
Dosages 0.1 mg/kg
Administration p.o.

Chemical lnformation & Solubility

Molecular Weight 333.43 Formula

C18H25N3O2.H2O
CAS No. 945667-22-1 SDF Download Saxagliptin hydrate SDF
Smiles C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N.O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (197.94 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 66 mg/mL

Water : 1 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

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