Drug intelligence / Profile preview

NF157

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal, Intravenous, Subcutaneous
01

Overview

NF157 is a small molecule purinergic receptor antagonist, notable for its potent and selective inhibition of the P2Y11 receptor (IC50 = 463 nM)[1][3][5]. It also displays selectivity for P2Y11 and P2X1 receptors over other purinergic subtypes[3][5]. Mechanistically, NF157 mitigates oxidized LDL-induced endothelial inflammation by blocking P2Y11-mediated signaling, which results in reduced expression of adhesion molecules (E-selectin, VCAM-1), suppression of reactive oxygen species production, inhibition of NADPH oxidase activity, and decreased pro-inflammatory cytokine secretion (IL-6, TNF-α)[2]. By blocking P2Y11 signaling, NF157 has shown protective effects against endothelial dysfunction associated with atherosclerosis in preclinical research[2]. It is primarily used as a research tool compound and there is currently no evidence that it has entered clinical trials or is under pharmaceutical development.

02

Targets

P2RY11 (Purinergic receptor P2Y11)P2RX1 (Purinergic receptor P2X 1)

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