NPY Y₁ receptor Antagonist

BIBO3304, a chemical probe, is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC₅₀=0.38 and 0.72 nM, respectively).

BIBP3226 TFA is a potent and selective neuropeptide Y Y1 (NPY Y1) and neuropeptide FF (NPFF) receptor antagonist, with K_is of 1.1, 79, and 108 nM for rNPY Y1, hNPFF2, and rNPFF, respectively. BIBP3226 TFA displays anxiogenic-like effect.

RF9 is a potent and selective Neuropeptide FF receptor antagonist, with K_i values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.

BMS-193885 is a selective neuropeptide Y1 receptor antagonist (K_i=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases.

NTNCB (Compound 11) hydrochloride is a potent and selective neuropeptide Y Y5 (NPY Y5) receptor antagonist with a K_i of 8 nM against human Y5.

RF9 hydrochloride is a potent and selective Neuropeptide FF receptor antagonist, with K_i values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively.

Neuropeptide Y Y1 receptor antagonist 1 (compound 39), a fluorescent probe, is a potent antagonist of neuropeptide Y Y¹ receptor (Y¹R), with a K_i of 0.19 nM.

J-115814 is a potent and selective neuropeptide Y1 antagonist with K_i values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors.