1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Trelagliptin succinate

Trelagliptin succinate (Synonyms: SYR-472 succinate)

Cat. No.: HY-15408A Purity: 99.89%
Handling Instructions

Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM).

For research use only. We do not sell to patients.

Trelagliptin succinate Chemical Structure

Trelagliptin succinate Chemical Structure

CAS No. : 1029877-94-8

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10 mM * 1 mL in DMSO USD 55 In-stock
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10 mg USD 80 In-stock
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50 mg USD 120 In-stock
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100 mg USD 160 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Trelagliptin (SYR-472) succinate is a potent, orally active and highly selective DPP-4 inhibitor with an IC50 of 4 nM. Trelagliptin succinate improves glycemic control in vivo and can be used for the study of type 2 diabetes mellitus (T2DM)[1].

IC50 & Target

IC50: 4 nM (DPP-4)[1]

In Vitro

Dipeptidyl peptidase-4 (DPP-4) is one of the widely explored novel targets for type 2 diabetes mellitus (T2DM) strategy to preserve the endogenous glucagon like peptide (GLP)-1 activity by inhibiting the DPP-4 action[1].
Trelagliptin exhibits potent inhibitory activity toward DPP-4 prepared from Caco-2 cells with an IC50 value of 5.4 nM. Trelagliptin also inhibits human, dog, and rat plasma DPP-4 activity with IC50 values of 4.2 nM, 6.2 nM, and 9.7 nM, respectively[2].
Trelagliptin is highly selective for DPP-4 and displays IC50 values >100,000 nM corresponding to >10,000-fold selectivity over DPP-2, DPP-8, DPP-9, PEP and FAPα activities. Trelagliptin shows DPP4 selective about 4- and 12-fold more potent than alogliptin (HY-A0023) and sitagliptin (HY-13749), respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Trelagliptin (oral gavage; 7 mg/kg; single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h[1].
Trelagliptin (oral gavage; 3 mg/kg; single dose; 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC0−120min of 19.3% compared with the vehicle group in ob/ob mice[3].
Trelagliptin (oral gavage; 10 mg/kg; once a week; 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-fold in AUC0−120min in ob/ob mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR ob/ob mice[3]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; once a week; 8 weeks
Result: Exerted chronic antidiabetic effects on type 2 diabetic db/db Mice.
Clinical Trial
Molecular Weight

475.47

Formula

C₂₂H₂₆FN₅O₆

CAS No.

1029877-94-8

SMILES

O=C(C=C(N1C[[email protected]](N)CCC1)N2CC3=C(C#N)C=CC(F)=C3)N(C)C2=O.O=C(O)CCC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (210.32 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (105.16 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1032 mL 10.5159 mL 21.0318 mL
5 mM 0.4206 mL 2.1032 mL 4.2064 mL
10 mM 0.2103 mL 1.0516 mL 2.1032 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.89%

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Keywords:

TrelagliptinSYR-472SYR472SYR 472Dipeptidyl PeptidaseDPPAnti-diabetic DiabetemellitusZafatekglycemicInhibitorinhibitorinhibit

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Trelagliptin succinate
Cat. No.:
HY-15408A
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