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Sitagliptin

Cat. No. M5965
Sitagliptin Structure
Synonym:

MK0431

Size Price Availability Quantity
Free Sample (1-2 mg)  USD 0 In stock
50mg USD 40  USD40 In stock
100mg USD 55  USD55 In stock
200mg USD 70  USD70 In stock
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Quality Control & Documentation
Biological Activity

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

Product Citations
Chemical Information
Molecular Weight 407.31
Formula C16H15F6N5O
CAS Number 486460-32-6
Solubility (25°C) DMSO 50 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] Hartley P, et al. Drugs Aging. Efficacy and Tolerability of Sitagliptin Compared with Glimepiride in Elderly Patients with Type 2 Diabetes Mellitus and Inadequate Glycemic Control: A Randomized, Double-Blind, Non-Inferiority Trial.

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