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Saxagliptin

Cat. No. M3435
Saxagliptin Structure
Synonym:

BMS-477118

Size Price Availability Quantity
10mg USD 98  USD98 In stock
25mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active inhibitor of dipeptidyl peptidase 4 (DPP-4) (Ki = 0.6-1.3 nM). Saxagliptin can be used in type 2 diabetes studies.

Protocol (for reference only)
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
Chemical Information
Molecular Weight 315.41
Formula C18H25N3O2
CAS Number 361442-04-8
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] No authors listed. Saxagliptin

[2] Carol Pollock, et al. Albuminuria-lowering effect of dapagliflozin alone and in combination with saxagliptin and effect of dapagliflozin and saxagliptin on glycaemic control in patients with type 2 diabetes and chronic kidney disease (DELIGHT): a randomised, double-blind, plac䲧畸Ỵ畹㧀畷羹皖

[3] No authors listed. Saxagliptin

[4] Dirk Mller-Wieland, et al. Efficacy and safety of dapagliflozin or dapagliflozin plus saxagliptin versus glimepiride as add-on to metformin in patients with type 2 diabetes

[5] Benjamin M Scirica, et al. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes mellitus

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Keywords: Saxagliptin, BMS-477118 supplier, Dipeptidyl Peptidase, inhibitors, activators


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