Home Proteases DPP inhibitor Trelagliptin succinate For research use only.

Trelagliptin succinate

Synonyms: SYR472

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 Chemical Structure

Trelagliptin succinate Chemical Structure

CAS No. 1029877-94-8

Purity & Quality Control

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

Trelagliptin succinate Related Products

Signaling Pathway

DPP Signaling Pathways

DPP Signaling Pathway

Biological Activity

Description 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).
Targets
DPP-4 [1]
(Cell-free assay)
4 nM
In vitro
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02372097 Completed
Healthy
Takeda
 March 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 475.47 Formula

C18H20FN5O2.C4H6O4
CAS No. 1029877-94-8 SDF --
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 95 mg/mL

Ethanol : 5 mg/mL


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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