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Saxagliptin

Cat. No. M3435

Saxagliptin Structure

Synonym: BMS-477118

Size Price Availability Quantity
10mg USD 240 In stock
25mg USD 500 In stock
100mg USD 1050 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Saxagliptin (Onglyza) is a new dipeptidyl peptidase-4 (DPP-4) inhibitor with IC50 of 50 nM. BI 1356 inhibited DPP-4 activity in vitro with an IC (50) of approximately 1 nM, compared with sitagliptin (19 nM), alogliptin (24 nM), saxagliptin (50 nM), and vildagliptin (62 nM). BI 1356 was a competitive inhibitor, with a K (i) of 1 nM.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male 13−14 week-old ob/ob mice
Formulation Water
Dosages 10 μmol/kg
Administration Orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 315.41
Formula C18H25N3O2
CAS Number 361442-04-8
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
Related DPP-4 Products
Teneligliptin HCl

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Teneligliptin

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Sitagliptin

Sitagliptin(MK 0431) is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Saxagliptin hydrate

Saxagliptin H2O is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Anagliptin

Anagliptin is a potent and selective DPP-4 inhibitor(IC50= 3.8 nM); > 10 fold less potent for DPP-8 and DPP-9.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Saxagliptin, BMS-477118 supplier, DPP-4, inhibitors

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