Other grades of this product :
| Saxagliptin hydrate Basic information |
| Product Name: | Saxagliptin hydrate | | Synonyms: | 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, hydrate (1:1), (1S,3S,5S)-;Saxagliptin hydrate;Saxagliptin hydrate
Unii-9gb927lajw;(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate;Saxagliptin hydrate
(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate;CS-1180;BMS 477118 hydrate;BMS477118 hydrate | | CAS: | 945667-22-1 | | MF: | C18H27N3O3 | | MW: | 333.43 | | EINECS: | 641-082-3 | | Product Categories: | Saxagliptin hydrate;API | | Mol File: | 945667-22-1.mol |
| Saxagliptin hydrate Chemical Properties |
| Melting point | 106-108°C | | storage temp. | -20°C Freezer | | solubility | DMSO (Slightly), Methanol (Sparingly) | | form | Solid | | color | White to Off-White |
| Saxagliptin hydrate Usage And Synthesis |
| Description | While liraglutide targets the incretin system as a GLP-1 analog for
therapeutic intervention in T2DM, saxagliptin enhances GLP-1 plasma concentrations by inhibiting the DPP-4 enzyme responsible for degradation of
GLP-1 by cleavage of the two N-terminal amino acids adjacent to alanine (or
proline), thereby rendering the hormone inactive.
Similarto vildagliptin,
saxagliptin is a cyanopyrrolidine substrate-based inhibitor. The proline
mimetic occupies the small S1-pocket while the nitrile’s trajectory aligns
with the scissile bond of the substrate. The slow dissociation kinetics of
saxagliptin is attributed to a reversible, covalent reaction between the nitrile
and the catalytically active serine hydroxyl (Ser630).
The steric bulk provided by the adamantyl moiety and the constrained cyclopropyl ring stabilizes the trans-rotamer of the amide, thereby preventing the problematic
intramolecular cyclization, via the amino group attacking the nitrile, which
is favored in the cis-conformation. Since metabolism of saxagliptin is primarily mediated by CYP3A4/5, there is a potential for drug interactions with concomitant administration of strong inducers or inhibitors of these cytochrome P450 enzymes. The most common adverse events (>5% of patients) included upper respiratory tract infection, urinary tract infection, and headache. | | Originator | Bristol-Myers-Squibb (US) | | Uses | Saxagliptin Hydrate is a selective and reversible dipeptidyl peptidase-4 (DPP4) inhibitor that may be used to develop treatment for type 2 diabetes. | | Definition | ChEBI: A hydrate that is the monohydrate form of anhydrous saxagliptin. Used for the treatment of Type II diabetes. | | Brand name | Onglyza |
| Saxagliptin hydrate Preparation Products And Raw materials |
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