BIIE 0246
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BIIE 0246是一种强效的和选择性的神经肽Y Y2受体拮抗剂,IC50值为3.3 nM [1].
神经肽Y Y2受体(Y2R)是一种神经肽Y (NPY)的G-蛋白偶联受体,其广泛分布在外围和中枢神经系统中.Y2R介导突触前抑制作用[2].
BIIE 0246是一种强效的和选择性的Y2R拮抗剂.在大鼠海马切片中,BIIE0246 (100 nM)抑制NPY和[ahx5-24]NPY诱发的原发性后放电活性.另外,BIIE0246抑制NPY和 [ahx5-24]NPY的抑制作用,其抑制由CA1区辐射层刺激诱发的群体兴奋性突触后电位(pEPSP).在转染大鼠Y2受体的HEK293细胞中,BIIE0246对特异性PYY3-36结合位点具有高亲和力,Ki值为8-15 nM.在大鼠结肠中,BIIE0246(1 μM)完全阻滞PYY3-36诱发的收缩反应[3].
在大鼠中,BIIE0246 (1 nM)减弱由PYY(3-36) (7.5 nmol/kg)诱发的摄食减少.在酒足饭饱的大鼠中,BIIE0246显著增加摄食.这些结果表明,Y2R对餐后饱腹感起着关键作用[4].在高架十字迷宫模型中,BIIE0246具有抗焦虑样效果[5].
参考文献：
[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.
| Physical Appearance | White solid |
| Storage | Store at 4°C |
| M.Wt | 896.06 |
| Cas No. | 246146-55-4 |
| Formula | C49H57N11O6 |
| Solubility | <67.2mg/ml in DMSO; <23.55mg/ml in ethanol |
| 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 |
| SDF | Download SDF |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
