Ki: 25.7 nM for Y1
Neuropeptide Y (NPY), a 36-residue peptide amide isolated originally from porcine brain, is a member of homologous hormone family including peptide YY (PYY) and pancreatic polypeptide (PP). It is the most abundant peptide in the mammalian brain and has been shown to exhibit a wide spectrum of central and peripheral activities. These actions are mediated by at least six G-protein coupled receptor subtypes denoted as Y1, Y2, Y3, Y4, Y5, and y6. BVD 10 is a highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists.
In vitro: The inability to form such hydrogen bonding in BVD 10 may prevent or perturb the C-terminus reverse turn, which may contribute, at least in part, to the increased Y1 selectivity . Moreover, BVD 10 and its NPY analogue peptide BVD15 were characterized conformationally. The two peptides exhibit different secondary structure characteristics in trifluoroethanol. Molecular modeling studies suggested that the C-terminus Tyr9 is oriented in different directions in the two peptides. The difference in the structures observed may contribute to the Y1 selectivity of BVD 10 relative to BVD 15 .
In vivo: No animal in vivo data have been reported so far.
Clinical trial: Up to now, BVD 10 is still in the preclinical development stage.
 Balasubramaniam A, Dhawan VC, Mullins DE, Chance WT, Sheriff S, Guzzi M, Prabhakaran M, Parker EM. Highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists based on [Pro(30), Tyr(32), Leu(34)]NPY(28-36)-NH2 (BW1911U90). J Med Chem. 2001 May 10;44(10):1479-82.
 Jois SD, Balasubramaniam A. Conformation of neuropeptide Y receptor antagonists: structural implications in receptor selectivity. Peptides. 2003 Jul;24(7):1035-43.
|Physical Appearance||White lyophilised solid|
|Storage||Desiccate at -20°C|
|Solubility||Soluble to 1 mg/ml in H2O|
|Canonical SMILES||CC[[email protected]]([[email protected]@](N)([H])/C(O)=N/[[email protected]@](C(N1CCC[[email protected]@]1([H])/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](C(OC)=O)([H])CC2=CC=C(O)C=C2)([H])CCCNC(N)=N)([H])CC(C)C)([H])CCCNC(N)=N)([H])CC3=CC=C(O)C=C3)([H])[[email protected]@](CC)([H])C)=O)(|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|