BIIE 0246 - CAS 246146-55-4
Catalog number: 246146-55-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C49H57N11O6
Molecular Weight:
896.05
COA:
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Targets:
Neuropeptide Y receptor
Description:
BIIE 0246 is a potent, selective and non-peptide antagonist which binds to the neuropeptide Y Y2 receptor (IC50 = 15 nM) with > 650-fold selectivity over Y1, Y4 and Y5 receptors.
Purity:
>98 %
Appearance:
Solid powder
Synonyms:
(2S)-5-(diaminomethylideneamino)-N-[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]-2-[[2-[1-[2-oxo-2-[4-(6-oxo-5,11-dihydrobenzo[c][1]benzazepin-11-yl)piperazin-1-yl]ethyl]cyclopentyl]acetyl]amino]pentanamide; BIIE-0246; BIIE 0246; BIIE-0246; CHEMBL540989; GTPL1547; CTK8E9439; BIIE0246
Solubility:
Soluble to 25 mM in ethanol and to 75 mM in DMSO
MSDS:
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InChIKey:
RSJAXPUYVJKAAA-JPGJPTAESA-N
InChI:
1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45(64)52-26-27-58-47(65)59(34-14-3-1-4-15-34)60(48(58)66)35-16-5-2-6-17-35)54-41(61)32-49(23-11-12-24-49)33-42(62)56-28-30-57(31-29-56)43-36-18-7-8-19-37(36)44(63)55-39-21-10-9-20-38(39)43/h1-10,14-21,40,43H,11-13,2
Canonical SMILES:
C1CCC(C1)(CC(=O)NC(CCCN=C(N)N)C(=O)NCCN2C(=O)N(N(C2=O)C3=CC=CC=C3)C4=CC=CC=C4)CC(=O)N5CCN(CC5)C6C7=CC=CC=C7C(=O)NC8=CC=CC=C68
1.Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening.
Brothers SP;Saldanha SA;Spicer TP;Cameron M;Mercer BA;Chase P;McDonald P;Wahlestedt C;Hodder PS Mol Pharmacol. 2010 Jan;77(1):46-57. doi: 10.1124/mol.109.058677. Epub 2009 Oct 16.
The role of neuropeptide Y Y2 receptor (Y2R) in human diseases such as obesity, mood disorders, and alcoholism could be better resolved by the use of small-molecule chemical probes that are substantially different from the currently available Y2R antagonist, 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) (BIIE0246). Presented here are five potent, selective, and publicly available Y2R antagonists identified by a high-throughput screening approach. These compounds belong to four chemical scaffolds that are structurally distinct from the peptidomimetic BIIE0246. In functional assays, IC(50) values between 199 and 4400 nM against the Y2R were measured, with no appreciable activity against the related NPY-Y1 receptor (Y1R). Compounds also displaced radiolabeled peptide YY from the Y2R with high affinity (K(i) values between 1.55 and 60 nM) while not displacing the same ligand from the Y1R. In contrast to BIIE0246, Schild analysis with NPY suggests that two of the five compounds behave as competitive antagonists. Profiling against a panel of 40 receptors, ion channels, and transporters found in the central nervous system showed that the five Y2R antagonists demonstrate greater selectivity than BIIE0246.
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