[CAS NO. 945667-22-1] Saxagliptin hydrate

Name: Saxagliptin hydrate
Brand: Arctom Scientific
SKU: SLK-S4697

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PRODUCTS SPECIFICATIONS [945667-22-1]

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Catalog

SLK-S4697

Brand

Selleck

CAS

945667-22-1

DESCRIPTION [945667-22-1]

Overview

MDL	-
Molecular Weight	333.43
Molecular Formula	C18H25N3O2.H2O
SMILES	[C@H](C(=O)N1[C@@H]2[C@@H](C2)C[C@H]1C#N)(N)C34CC5(O)CC(C3)CC(C4)C5.O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.9991 mL	14.9957 mL	29.9913 mL
5 mM	0.5998 mL	2.9991 mL	5.9983 mL
10 mM	0.2999 mL	1.4996 mL	2.9991 mL
50 mM	0.0600 mL	0.2999 mL	0.5998 mL

Description

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

Targets

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.

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.

References

[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.

Synonyms

2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.1^3,7]dec-1-yl)acetyl]-, hydrate (1:1), (1S,3S,5S)-

Saxagliptin hydrate

Saxagliptin monohydrate