BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. It reduces food intake and body weight via central Y1 inhibition and is brain penetrant. BMS-193885 has 3.3 nM affinity at the neuropeptide Y(1) receptor, acting competitively at the neuropeptide Y binding site. BMS-193885 increased the K(d) of [(125)I]PeptideYY from 0.35 nM to 0.65 nM without changing the B(max) (0.16 pmol/mg of protein) in SK-N-MC cells that endogenously express the neuropeptide Y(1) receptor. It is also found to be a full antagonist with an apparent K(b) of 4.5 nM measured by reversal of forskolin (FK)-stimulated inhibition of cAMP production by neuropeptide Y.
Cat.No
DC74848
Name
BMS193885 free base
Chemical Properties
CAS
186185-03-5
Formula
C33H42N4O6
MW
590.71
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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