| BIIE 0246NPY Y2 receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
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Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.00%
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| Cas No. | 246146-55-4 | SDF | Download SDF |
| Chemical Name | (S)-5-((diaminomethylene)amino)-N-(2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl)-2-(2-(1-(2-oxo-2-(4-((S)-6-oxo-6,11-dihydro-5H-dibenzo[b,e]azepin-11-yl)piperazin-1-yl)ethyl)cyclopentyl)acetamido)pentanamide | ||
| Canonical SMILES | O=C(CC1(CC(N[C@H](C(NCCN2C(N(C3=CC=CC=C3)N(C4=CC=CC=C4)C2=O)=O)=O)CCC/N=C(N)N)=O)CCCC1)N5CCN([C@@H](C6=CC=CC=C67)C8=CC=CC=C8NC7=O)CC5 | ||
| Formula | C49H57N11O6 | M.Wt | 896.06 |
| Solubility | <67.2mg l="" in="" dmso;=""><23.55mg l="" in="" ethanol=""> | Storage | Store at -20°C |
| Physical Appearance | White solid | 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. | ||
BIIE 0246 is a potent and selective antagonist of neuropeptide Y Y2 receptor with IC50 value of 3.3 nM [1].
Neuropeptide Y Y2 receptor (Y2R) is a G-protein-coupled receptor for neuropeptide Y (NPY), which is widely distributed in the peripheral and central nervous system. Y2R mediates the presynaptic inhibitory effect [2].
BIIE 0246 is a potent and selective Y2R antagonist. In rat hippocampal slices, BIIE0246 (100 nM) suppressed the inhibition of primary afterdischarge activity induced by NPY and [ahx5-24]NPY. Also, BIIE0246 suppressed the inhibitory effects of NPY and [ahx5-24]NPY, which inhibited the population excitatory postsynaptic potential (pEPSP) evoked by stratum radiatum stimulation in area CA1 [2]. In HEK293 cells transfected with the rat Y2 receptor, BIIE0246 exhibited high affinity for specific PYY3-36 binding sites with Ki values of 8-15 nM. In the rat colon, BIIE0246 (1 μM) completely blocked PYY3-36-induced contraction response [3].
In rats, BIIE0246 (1 nM) attenuated the reduction in feeding induced by PYY(3-36) (7.5 nmol/kg). In satiated rats, BIIE0246 significantly increased feeding. These results suggested that Y2R played a critical role in post-prandial satiety [4]. In the elevated plus-maze, BIIE0246 exhibited anxiolytic-like effect [5].
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.
