Saxagliptin hydrate
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- CAS-Nr.
- 945667-22-1
- Englisch Name:
- Saxagliptin hydrate
- Synonyma:
- CS-1180;Onglyza hydrate;BMS477118 hydrate;BMS-477118 hydrate;BMS 477118 hydrate;Saxagliptin hydrate;Saxagliptin hydrate
Unii-9gb927lajw;Saxagliptin hydrate (BMS-477118 hydrate);BMS-477118 HYDRATE;BMS 477118 HYDRATE;BMS477118 HYDRATE;4-trifluorosulfoyl-3'-trifluoroacetamino-4-demethyldaunorubicin
- CBNumber:
- CB92542796
- Summenformel:
- C18H27N3O3
- Molgewicht:
- 333.43
- MOL-Datei:
- 945667-22-1.mol
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Saxagliptin hydrate Eigenschaften
- Schmelzpunkt:
- 106-108°C
- storage temp.
- -20°C Freezer
- Löslichkeit
- DMSO (Slightly), Methanol (Sparingly)
- Aggregatzustand
- Solid
- Farbe
- White to Off-White
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitsschädlich bei Verschlucken. |
Akute Toxizität oral |
Kategorie 4 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizität (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
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| Sicherheit |
| P261 |
Einatmen von Staub vermeiden. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen. |
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Saxagliptin hydrate Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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.
Verwenden
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: Saxagliptin hydrate is a hydrate that is the monohydrate form of anhydrous saxagliptin. Used for the treatment of Type II diabetes. It has a role as a hypoglycemic agent and an EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor. It contains a saxagliptin.
Biologische Aktivität
Saxagliptin (BMS-477118) is an orally active, highly potent and long-acting dipeptidyl peptidase IV inhibitor (human DPP-IV Ki = 0.9 nM; plasma DDP-IV inhibition = 87% 0.5-4h post 4 μmol/kg po. in normal rats) with therapeutic efficacy against type 2 diabetes in vivo (plasma glucose clearance = 28/43/61% post 0.3/1.0/3.0 μmol/kg po. in Zucker fa/fa rats).
Saxagliptin hydrate Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Saxagliptin hydrate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 185)Lieferanten
- 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
- BMS-477118 hydrate
- BMS-477118 HYDRATE;BMS 477118 HYDRATE;BMS477118 HYDRATE
- Saxagliptin hydrate (BMS-477118 hydrate)
- Onglyza hydrate
- (1S,3S,5S)-2-((2S)-2-amino-2-(3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile hydrate
- (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
- Saxagliptin MonohydrateQ: What is
Saxagliptin Monohydrate Q: What is the CAS Number of
Saxagliptin Monohydrate Q: What is the storage condition of
Saxagliptin Monohydrate Q: What are the applications of
Saxagliptin Monohydrate
- (1S,3S,5S)-2-((2S)-2-Amino-2-(3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile monohydrate
- 4-trifluorosulfoyl-3'-trifluoroacetamino-4-demethyldaunorubicin
- 945667-22-1
- C18H25N3O2H2O
- Saxagliptin hydrate
- API
