| Identification | Back Directory | [Name]
BIIE 0246 | [CAS]
246146-55-4 | [Synonyms]
BIIE 0246
AR-H 053591
BIIE-0246;BIIE0246
N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-
(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
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
Cyclopentaneacetamide, 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]- | [Molecular Formula]
C49H57N11O6 | [MDL Number]
MFCD04113026 | [MOL File]
246146-55-4.mol | [Molecular Weight]
896.05 |
| Chemical Properties | Back Directory | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
<67.2mg/ml in DMSO; <23.55mg/ml in ethanol | [form ]
solid | [pka]
13.28±0.40(Predicted) | [color ]
White | [InChIKey]
RSJAXPUYVJKAAA-JPGJPTAESA-N | [SMILES]
[n]2([n]([c]([n]([c]2=O)CCNC(=O)[C@@H](NC(=O)CC8(CCCC8)CC(=O)N4CCN(CC4)C5c6c(cccc6)NC(=O)c7c5cccc7)CCCNC(=N)N)=O)c3ccccc3)c1ccccc1 |
| Hazard Information | Back Directory | [Uses]
BIIE 0246, is a selective non-peptide antagonist which binds to the neuropeptide NPY2-R in a competitive manner. Studies have also shown that BIIE 0246 is highly lipophilic and as a result BIIE 0246 builds up at membranes near the receptors. | [Biological Activity]
Potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y 2 receptor (IC 50 = 15 nM). Displays > 650-fold selectivity over Y 1 , Y 4 and Y 5 receptors. Active in vivo . | [in vivo]
BIIE-0246 (1.3 mg/kg; I.p.; daily for 2 or 4.5 weeks) prevents diet-induced obesity in OE-NPYDβH mice, but enhances obesity in WT Mice[1].
BIIE-0246 (10 μg/day; i.p.; daily for 14 days) reduces albuminuria in ADR (adriamycin) nephropathy[3]. | Animal Model: | Homozygous transgenic male OE-NPYDβH and WT C57Bl/6N mice[1] | | Dosage: | 1.3 mg/kg | | Administration: | I.p.; daily for 2 or 4.5 weeks | | Result: | Increased body weight gain in both genotypes on the chow diet caused metabolic disturbances, especially in WT mice. During energy surplus (i.e., on Western diet), blocking of Y2-receptors induced obesity in WT mice and OE-NPYDβH mice showed a reduced fat mass gain, hepatic glycogen and serum cholesterol levels relative to body adiposity. |
| Animal Model: | Male BALB/c mice[3] | | Dosage: | 10 μg/day | | Administration: | I.p.; daily for 14 days | | Result: | Reduces albuminuria in ADR nephropathy. |
| [IC 50]
NPY Y2 receptor: 15±3 nM (IC50) | [References]
[1]. doods h, gaida w, wieland ha, et al. biie0246: a selective and high affinity neuropeptide y y(2) receptor antagonist. eur j pharmacol, 1999, 384(2-3): r3-5.
[2]. el bahh b, cao jq, beck-sickinger ag, et al. blockade of neuropeptide y(2) receptors and suppression of npy's anti-epileptic actions in the rat hippocampal slice by biie0246. br j pharmacol, 2002, 136(4): 502-509.
[3]. dumont y, cadieux a, doods h, et al. biie0246, a potent and highly selective non-peptide neuropeptide y y(2) receptor antagonist. br j pharmacol, 2000, 129(6): 1075-1088.
[4]. abbott cr, small cj, kennedy ar, et al. blockade of the neuropeptide y y2 receptor with the specific antagonist biie0246 attenuates the effect of endogenous and exogenous peptide yy(3-36) on food intake. brain res, 2005, 1043(1-2): 139-144.
[5]. bacchi f, mathé aa, jiménez p, et al. anxiolytic-like effect of the selective neuropeptide y y2 receptor antagonist biie0246 in the elevated plus-maze. peptides, 2006, 27(12): 3202-3207. |
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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Merck KGaA
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www.sigmaaldrich.cn |
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