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Saxagliptin hydrate

Catalog No. T0178 CAS 945667-22-1

Synonyms: Onglyza hydrate, BMS-477118 hydrate

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

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Saxagliptin hydrate, CAS 945667-22-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 50.00
10 mg	In stock	$ 65.00
25 mg	In stock	$ 121.00
50 mg	In stock	$ 219.00
100 mg	In stock	$ 359.00
500 mg	In stock	$ 863.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.8%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).
Targets&IC50	DPP4:26 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].
Cell Research	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). (Only for Reference)

Synonyms	Onglyza hydrate, BMS-477118 hydrate
Molecular Weight	333.43
Formula	C18H25N3O2·H2O
CAS No.	945667-22-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 61 mg/mL (182.9 mM)

H2O: 1 mg/mL (3 mM)

Ethanol: 61 mg/mL (182.9 mM)

References and Literature

1. Neumiller JJ, et al. Am J Health Syst Pharm. 2010, 67(18):1515-25. 2. Solini A, et al. Vascul Pharmacol. 2016, 76:62-71. 3. Henry RR, et al. Diabetes Obes Metab. 2011, 13(9):850-8. 4. Sbaraglini ML, et al. Eur J Pharmacol. 2014, 727:8-14.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Highly Selective Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Protease Inhibitor Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library Anti-Diabetic Compound Library Bioactive Compounds Library Max Glycometabolism Compound Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Saxagliptin hydrate 945667-22-1 Proteases/Proteasome Ubiquitination DPP-4 Proteasome DPP glucagon-like c-myc BMS-477118 glucagon β-catenin BMS 477118 Saxagliptin BMS477118 insulin Onglyza hydrate proliferation Onglyza Hydrate p-AKT Inhibitor peptide-1 BMS-477118 Hydrate BMS-477118 hydrate diabetes Dipeptidyl Peptidase Saxagliptin Hydrate BMS477118 Hydrate inhibit BMS 477118 Hydrate inhibitor

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