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BIIE0246

Chemical Structure : BIIE0246

CAS No.: 246146-55-4

BIIE0246 (BIIE 0246, BIIE-0246)

Catalog No.: PC-38252Not For Human Use, Lab Use Only.

BIIE0246 (BIIE 0246) is a potent, highly selective non-peptide neuropeptide Y Y2 receptor antagonist with IC50 of 15 nM, >650-fold selectivity over Y1, Y4 and Y5 receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BIIE0246 (BIIE 0246) is a potent, highly selective non-peptide neuropeptide Y Y2 receptor (NPY2R) antagonist with IC50 of 15 nM, >650-fold selectivity over Y1, Y4 and Y5 receptors.
BIIE0246 (1 uM) completely blocked the contraction induced by PYY(3-36), but not that of [Leu(31), Pro(34)]NPY (a Y(1), Y(4) and Y(5) agonist) and hPP (a Y(4) and Y(5) agonist).
BIIE0246 displaced [125I]neuropeptide Y with high affinity (IC(50)=3.3 nM) from the human neuropeptide Y Y(2) receptor and proved to be highly selective.

Physicochemical Properties

M.Wt 896.066
Formula C49H57N11O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide

References

1. Doods H,et al. Eur J Pharmacol. 1999 Nov 19;384(2-3):R3-5.

2. Malmström RE. Br J Pharmacol. 2001 Aug;133(7):1073-80.

3. Goumain M, et al. Mol Pharmacol. 2001 Jul;60(1):124-34.

4. Smith-White MA, et al. Br J Pharmacol. 2001 Feb;132(4):861-8.

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