Home Proteases DPP inhibitor Trelagliptin succinate

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Trelagliptin succinate DPP inhibitor

Cat.No.S5063

Trelagliptin succinate (SYR472) is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM).
Trelagliptin succinate DPP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 475.47

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Quality Control

Batch: S506301 DMSO]95 mg/mL]false]Water]95 mg/mL]false]Ethanol]5 mg/mL]false Purity: 99.96%
99.96

Chemical Information, Storage & Stability

Molecular Weight 475.47 Formula

C18H20FN5O2.C4H6O4

 Storage (From the date of receipt)
CAS No. 1029877-94-8 -- Storage of Stock Solutions

Synonyms SYR472 Smiles CN1C(=O)C=C(N(C1=O)CC2=C(C=CC(=C2)F)C#N)N3CCCC(C3)N.C(CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (199.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 95 mg/mL

Ethanol : 5 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
DPP-4 [1]
(Cell-free assay)
4 nM
In vitro
Trelagliptin is selective over other related DPP enzymes, P450 enzymes and hERG channel[1]. It 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[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02372097 Completed
Healthy
Takeda
 March 2015 Phase 1

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