Human enteropeptidase-IN-1_product_DataBase

Bioactivity	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].
Target	IC50(initial): 20 nM (enteropeptidase)IC50(app): 1.2 nM (enteropeptidase)
Invitro	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.)
Name	Human enteropeptidase-IN-1
CAS	1802891-23-1
Formula	C20H18N4O7
Molar Mass	426.38
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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