Saxagliptin (BMS-477118) - Moligand™, 10mM in DMSO , Inhibitor of dipeptidyl peptidase 4, CAS No.361442-04-8, Inhibitor of dipeptidyl peptidase 4

CAS: 361442-04-8 Cat. No.: S408204 Formula: C₁₈H₂₅N₃O₂ Peso molecolare: 315.41 Numero EC: 111-193-7 PubChem CID: 11243969

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Onglyza | 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

Saxagliptin (BMS-477118) Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
In vitro

Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with K_i of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9). Saxagliptin reduces the degradation of the incretin hormone Glukagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of Glukagon secretion.

In vivo

Maximal responses of Saxagliptin in glucose excursion in Zucker^fa/fa rats are associated with plasma DPP4 inhibition of approximately 60% vs. control, and no additional antihyperglycemic effects are seen at higher percent inhibition. Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT.
Cell Data

cell lines：MZ-CRC-1 and TT cells

Concentrations：

Incubation Time：

Powder Purity:≥96%

Specifications

Sinonimi

Onglyza | 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)-

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

INHIBITOR

Meccanismo d'azione

Inhibitor of dipeptidyl peptidase 4

Nomi e identificatori

Isomeri SMILES

C1[C@@H]2C[C@@H]2N([C@@H]1C#N)C(=O)[C@H](C34CC5CC(C3)CC(C5)(C4)O)N

PubChem CID

11243969

Peso molecolare

315.41

Obiettivi associati (umani)

DPP4 Tclin Dipeptidyl peptidase 4 (15 Activities)

Discover Target: DPP4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DPP8 Tchem Dipeptidyl peptidase 8 (3 Activities)

Discover Target: DPP8

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DPP9 Tchem Dipeptidyl peptidase 9 (3 Activities)

Discover Target: DPP9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 100 mg/mL (123.18 mM); Water: 100 mg/mL (123.18 mM); Ethanol: 100 mg/mL (123.18 mM)

Domande frequenti

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 361442-04-8, the molecular formula is C18H25N3O2, and the molecular weight is 315.41 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.