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Anagliptin

Cat. No. M5417
Anagliptin Structure
Synonym:

SK-0403

Size Price Availability Quantity
5mg USD 154  USD154 In stock
10mg USD 264  USD264 In stock
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Quality Control & Documentation
Biological Activity

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

Chemical Information
Molecular Weight 383.45
Formula C19H25N7O2
CAS Number 739366-20-2
Solubility (25°C) 36 mg/mL in DMSO
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] Yang HK, et al. Endocr J. A randomized, placebo-controlled, double-blind, phase 3 trial to evaluate the efficacy and safety of anagliptin in drug-naïve patients with type 2 diabetes.

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