Saxagliptin hydrate

SKU: orb1310866

Description

Saxagliptin hydrate, also known as Onglyza hydrate, is a potent and selective reversible inhibitor of dipeptidyl peptidase-4 (DPP-4) with an IC50 of 26 nM and a Ki of 1.3 nM. This compound is widely used in diabetes research to study DPP-4's role in glucose metabolism, employing both in vitro enzymatic assays and in vivo models of type 2 diabetes.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 945667-22-1
• MW: 333.43
• Purity: 99.80% (May vary between batches)
• Formula: C₁₈H₂₅N₃O₂·H₂O
• SMILES: O.N[C@H](C(=O)N1[C@H]2C[C@H]2C[C@H]1C#N)C12CC3CC(CC(O)(C3)C1)C2
• Target: DPP-4,Proteasome
• Solubility: H2O:1 mg/mL (3 mM);DMSO:70 mg/mL (209.94 mM);Ethanol:61 mg/mL (182.95 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6 mM)

Bioactivity

• Target IC50:
  DPP4:26 nM
• In Vivo:
  Saxagliptin exerts direct beneficial effects on the arterial wall in an animal model of type 2 diabetes by increasing NO availability and improving antioxidant status. Saxagliptin reverses vascular hypertrophic remodeling and ameliorates NO availability in small arteries from db/db mice through the abrogation of NAD(P)H oxidase-driven eNOS uncoupling and by reducing the action of cyclooxygenase-1-derived vasoconstrictors downregulating the expression of thromboxane-prostanoid receptors. DPP-4 inhibition with saxagliptin also improves pancreatic β-cell function in postprandial and fasting states, and decreases postprandial glucagon concentration.
• In Vitro:
  In vitro, saxagliptin inhibits FBS-, insulin- and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC and MC3T3E1 preosteoblasts. In the absence of growth factors, saxagliptin has no effect on ERK activation or cell proliferation. In both MSC and MC3T3E1 cells, saxagliptin in the presence of FBS inhibits Runx2 and osteocalcin expression, type-1 collagen production and mineralization, while increasing PPAR-gamma expression.
• Cell Research:
  Sub-confluent cells are serum-starved overnight and then incubated with 1.5 or 15 μM saxagliptin and/or FBS (1%), insulin (5 ng/mL) or IGF1 (10-8 M) for 24 h (effects on cell proliferation) or 1 h (effects on signal transduction mechanisms). (Only for Reference)

Storage & Handling

• Storage: 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

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

Compound Identifiers

PubChem CID

53297473