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Trelagliptin succinate

Cat. No. M8882
Trelagliptin succinate Structure

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.


[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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Keywords: Trelagliptin succinate, SYR472 succinate supplier, Dipeptidyl Peptidase, inhibitors, activators

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