Human enteropeptidase-IN-1

Names

[ CAS No. ]:
1802891-23-1

[ Name ]:
Human enteropeptidase-IN-1

Biological Activity

[Description]:

Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[Target]

IC50(initial): 20 nM (enteropeptidase)[1] IC50(app): 1.2 nM (enteropeptidase)[1]


[In Vitro]

Human enteropeptidase-IN-1 (compound 6b) has inhibitory activity against enteropeptidase with IC50(initial)* of 20 nM and IC50(app)** of 1.2 nM[1]. (*IC50(initial) refers to the inhibitory activity of human enteropeptidase after 6 min of incubation with the enzyme, substrate, and compound. **IC50(app) refers to the apparent IC50 value after 120 min of incubation with the enzyme, substrate, and compound.)

[References]

[1]. Ikeda Z, et al. Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity. J Med Chem. 2022 Jun 23;65(12):8456-8477.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H18N4O7

[ Molecular Weight ]:
426.38

Related Compounds