Saxagliptin

SKU: orb1300984

Description

Saxagliptin (BMS-477118) is a potent, reversible, and selective DPP-4 inhibitor exhibiting an IC50 of 26 nM. It is widely used in diabetes research to study glycemic control mechanisms in both cellular assays and animal models of type 2 diabetes.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 361442-04-8
• MW: 315.41
• Purity: 99.95%
• Formula: C₁₈H₂₅N₃O₂
• SMILES: [H][C@@]12C[C@]1([H])N([C@@H](C2)C#N)C(=O)[C@@H](N)[C@]12C[C@@]3([H])C[C@]([H])(C[C@](O)(C3)C1)C2
• Target: DPP-4,Proteasome
• Solubility: H2O:58 mg/mL (183.89 mM);DMSO:35 mg/mL (110.97 mM);Ethanol:23 mg/mL (72.92 mM)

Bioactivity

• Target IC50:
  DPP4:26 nM
• In Vivo:
  Maximal responses of Saxagliptin in glucose excursion in Zuckerfa/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.
• 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 Ki 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 glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-myc, diabetes, Dipeptidyl Peptidase, DPP, DPP4, DPP-4, BMS 477118, BMS477118, BMS-477118, Inhibitor, p-AKT, inhibit, Onglyza, insulin, glucagon-like, glucagon, β-catenin, Saxagliptin, proliferation, peptide-1

Compound Identifiers

PubChem CID

11235729