SAXAGLIPTIN

Synonyms. Saxagliptin; (1S,3S,5S)-2-((2S)-Amino(3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)acetyl)2- azabicyclo(3.1.0)hexane-3-carbonitrile; Onglyza;

SAXAGLIPTIN

 

PRODUCT IDENTIFICATION

CAS RN

361442-04-8 (anhydrous), 945667-22-1 (hydrate)

EINECS RN

  

FORMULA

C18H25N3O2

MOLE WEIGHT

 315.41

H.S CODE

 2933.99.7500

SMILES

 N1([C@H](CC2[C@H]1C2)C#N)C(=O)[C@@H](C12CC3CC(C1)(O)CC (C3)C2)N

CLASSIFICATION

Dipeptidyl-Peptidase IV Inhibitor, Hypoglycemic agent, Protease Inhibitor

EXTRA NOTES

 Putative antidiabetic agent for treating type 2 diabetes; inhibits DPP4 protein, human.
Treatment of Type II diabetes mellitus and metabolic syndrome

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE.

white powder

MELTING POINT

 

BOILING POINT

548 ~ 549 C

DENSITY

1.35

SOLUBILITY IN WATER

 

SOLVENT SOLUBILITY  

VAPOR DENSITY

 

log P(octanol-water)

  

VAPOR PRESSURE

  

AUTOIGNITION TEMP

  
pKa

 

REFRACTIVE INDEX

 

FLASH POINT

 

 

STABILITY AND REACTIVITY
STABILITY Stable under normal conditions.

INCOMPATIBLE MATERIALS

Strong oxidizing agents
POLYMERIZATION

Has not been reported

NFPA RATINGS

Health: 0, Flammability:0, Reactivity: 0

 

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking - Saxagliptin

Google Scholar Search - Saxagliptin

Drug Information Portal (U.S. National Library of Medicine) - Saxagliptin

PubChem Compound Summary - Saxagliptin

Drug Bank -  Saxagliptin

KEGG (Kyoto Encyclopedia of Genes and Genomes) - Saxagliptin

http://www.ebi.ac.uk/ - Saxagliptin

http://www.ncbi.nlm.nih.gov/ - Saxagliptin

http://toxnet.nlm.nih.gov/
Hazardous Substances Data Bank -  Saxagliptin

http://dailymed.nlm.nih.gov/
Mechanism of Action:Increased concentrations of the incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are released into the bloodstream from the small intestine in response to meals. These hormones cause insulin release from the pancreatic beta cells in a glucose-dependent manner but are inactivated by the DPP4 enzyme within minutes. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, reducing hepatic glucose production. In patients with type 2 diabetes, concentrations of GLP-1 are reduced but the insulin response to GLP-1 is preserved. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus.

http://www.biomedcentral.com/
Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

Local
Dipeptidyl peptidase-4 inhibitors

Product

CAS RN.

Alogliptin

 850649-61-5

Alogliptin benzoate

850649-62-6

Gemigliptin

911637-19-9

Linagliptin

 668270-12-0

Saxagliptin

361442-04-8

Saxagliptin hydrate

 945667-22-1

Sitagliptin

 486460-32-6

Vildagliptin

 274901-16-5

 

SALES SPECIFICATION

APPEARANCE

off-white to yellow powder

ASSAY

98.0% min

LOSS ON DRYING

5.0% max

HEAVY METALS

10ppm max

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

Not regulated

HAZARD CLASS

  
PACKING GROUP  

 

SAFETY INFORMATION

HAZARD OVERVIEW

Not known
HAZARD CODES

 

RISK PHRASES

  

SAFETY PHRASES

  

 

PACKING

 

 

PRICE INFORMATION