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NVP DPP 728 dihydrochloride

Names

[ CAS No. ]:
207556-62-5

[ Name ]:
NVP DPP 728 dihydrochloride

[Synonym ]:
3-Pyridinecarbonitrile, 6-[[2-[[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethyl]amino]ethyl]amino]-, hydrochloride (1:2)
6-{[2-({2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethyl}amino)ethyl]amino}nicotinonitrile dihydrochloride
6-{[2-({2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino}nicotinonitrile dihydrochloride

Biological Activity

[Description]:

NVP-DPP728 dihydrochloride is a potent, selective and orally active dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 11 nM. NVP-DPP728 dihydrochloride can be used for the research of diabetes mellitus[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase
Research Areas >> Metabolic Disease

[Target]

Ki: 11 nM (DPP-IV) [1]


[In Vivo]

NVP-DPP728 inhibits DPP-IV and improves insulin secretion and glucose tolerance, probably through augmentation of the effects of endogenous GLP-1[2]. Animal Model: Obese (fa/fa) and lean (FA/?) Zucker rats[2] Dosage: 3.715 mg/kg Administration: Oral administration Result: Led to inhibition of plasma DPP-IV activity.

[References]

[1]. T E Hughes, et al. NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)- pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV. Biochemistry. 1999 Sep 7;38(36):11597-603.

[2]. B Balkan, et al. Inhibition of dipeptidyl peptidase IV with NVP-DPP728 increases plasma GLP-1 (7-36 amide) concentrations and improves oral glucose tolerance in obese Zucker rats. Diabetologia. 1999 Nov;42(11):1324-31.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H20Cl2N6O

[ Molecular Weight ]:
371.265

[ Exact Mass ]:
370.107574

[ PSA ]:
108.07000

[ LogP ]:
1.82406


Related Compounds

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