For research use only.
Catalog No.S4697 Synonyms: BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate
CAS No. 945667-22-1
Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
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|Description||Saxagliptin H2O (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.|
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.
|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. DPP-4 inhibition with saxagliptin also improves pancreatic β-cell function in postprandial and fasting states, and decreases postprandial glucagon concentration.|
|In vitro||DMSO||66 mg/mL (197.94 mM)|
|Ethanol||66 mg/mL (197.94 mM)|
|Water||1 mg/mL (2.99 mM)|
* 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.
|Synonyms||BMS-477118 hydrate, Onglyza hydrate, BMS 477118 hydrate, BMS477118 hydrate|
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||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
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