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Trelagliptin succinate

Cat. No. M8882
Trelagliptin succinate Structure
Synonym:

SYR472 succinate

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
50mg USD 120  USD120 In stock
100mg USD 160  USD160 In stock
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Quality Control & Documentation
Biological Activity

Trelagliptin(SYR-472) succinate is selective over other related DPP enzymes, P450 enzymes and hERG channel. Trelagliptin(SYR-472) succinate exhibits approximately 4- and 12-fold more potent inhibition against human dipeptidyl peptidase-4 than alogliptin and sitagliptin, respectively, and >10,000-fold selectivity over related proteases including dipeptidyl peptidase-8 and dipeptidyl peptidase-9. Kinetic analysis reveals reversible, competitive and slow-binding inhibition of dipeptidyl peptidase-4 by trelagliptin (t1/2 for dissociation ≈ 30 minutes). X-ray diffraction data indicates a non-covalent interaction between dipeptidyl peptidase and trelagliptin.

Currently, all available DPP-4 inhibitors are dosed once-daily. Phase III clinical studies with trelagliptin in Japan to evaluate its safety and efficacy in a once-weekly oral treatment regimen.

Product Citations
Chemical Information
Molecular Weight 475.47
Formula C18H20FN5O2.C4H6O4
CAS Number 1029877-94-8
Solubility (25°C) DMSO 90 mg/mL
Water 90 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] Grimshaw CE, et al. PLoS One. Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism.

[2] Patel BD, et al. Eur J Med Chem. Recent approaches to medicinal chemistry and therapeutic potential of dipeptidyl peptidase-4 (DPP-4) inhibitors.

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