Trelagliptin Chemical Properties

Boiling point:

519.0±60.0 °C(Predicted)

Density 

1.38±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥11.6 mg/mL in DMSO; ≥3.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥93.8 mg/mL in H2O

form 

solid

pka

9.88±0.20(Predicted)

InChI

InChI=1S/C18H20FN5O2/c1-22-17(25)8-16(23-6-2-3-15(21)11-23)24(18(22)26)10-13-7-14(19)5-4-12(13)9-20/h4-5,7-8,15H,2-3,6,10-11,21H2,1H3/t15-/m1/s1

InChIKey

IWYJYHUNXVAVAA-OAHLLOKOSA-N

SMILES

C(#N)C1=CC=C(F)C=C1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1

Trelagliptin Usage And Synthesis

Uses

Trelagliptin is a highly selective, long-acting dipeptidyl peptidase IV (DPP-4) inhibitor. This inhibitor provides sustained reduction of plasma DPP-4 activity and lowering of blood glucose in animal models of diabetes.

Definition

ChEBI: Trelagliptin is a member of benzenes and a nitrile.

Biological Activity

trelagliptin (syr-472) is a selective inhibitor of dpp-4 and is developed for the treatment of type 2 diabetes mellitus (t2dm) [1].dipeptidyl peptidase (dpp)-4 also known as adenosine deaminase complexing protein 2 or cd26 is an antigenic enzyme that expressed on the surface of most cell types and plays an important role in regulating immune system, signal transduction and apoptosis [2, 3].trelagliptin (syr-472) is a potent dpp-4 inhibitor and can be administered once weekly which unlike its other class approved agents that be taken once daily [1]. in japan,

target

DPP-4

References

[1]. mckeage, k., trelagliptin: first global approval. drugs, 2015. 75(10): p. 1161-4.
[2]. inagaki, n., et al., once-weekly trelagliptin versus daily alogliptin in japanese patients with type 2 diabetes: a randomised, double-blind, phase 3, non-inferiority study. lancet diabetes endocrinol, 2015. 3(3): p. 191-7.
[3]. inagaki, n., et al., syr-472, a novel once-weekly dipeptidyl peptidase-4 (dpp-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. lancet diabetes endocrinol, 2014. 2(2): p. 125-32.

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