Home Proteases DPP inhibitor Saxagliptin hydrate

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Saxagliptin hydrate DPP inhibitor

Cat.No.S4697

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

Chemical Structure

Molecular Weight: 333.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 333.43 Formula

C18H25N3O2.H2O

 Storage (From the date of receipt)
CAS No. 945667-22-1 Download SDF Storage of Stock Solutions

Synonyms BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate Smiles C1C2CC2N(C1C#N)C(=O)C(C34CC5CC(C3)CC(C5)(C4)O)N.O

Solubility

In vitro
Batch:

DMSO : 66 mg/mL (197.94 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 66 mg/mL

Water : 1 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% 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.

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
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].
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].
References

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