GlpBio

BIIE 0246

目录号: GC17424纯度: >98%同义词: AR-H 053591
COASDSData Sheet
BIIE 0246 是一种有效且高度选择性的非肽神经肽 Y (NPY) Y2 受体拮抗剂，IC50 为 15 nM。
BIIE 0246
Cas No.: 246146-55-4
规格价格库存数量操作
1mg¥1,103.00现货
1
10mg¥2,352.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

Animal experiment:

Mice[2]Homozygous transgenic male OE-NPYDbH and WT mice are used. The mice are housed at 21±3°C with a 12-h light/12-h dark cycle. To study the effect of Y2-receptor antagonism in healthy conditions, standard rodent chow is fed ad libitum to OE-NPYDbH (NPY) and WT mice. To study the effect in DIO, western diet is fed for 8 weeks prior to the drug administration. Drug treatment is studied at the age of 20 weeks. Prior to treatments the mice are habituated for 2 weeks to the handling stress with daily saline injections (i.p). Mice receive 1.3 mg/kg of Y2-receptor antagonist (BIIE-0246) or vehicle with daily IP injections. At termination, mice are fasted for 3 h and blood glucose is measured from awake animals. Mice are then anesthetized with ketamine (75 mg/kg i.p) and medetomidine (1 mg/kg i.p). Subcutaneous, epididymal, retroperitoneal and mesenteric white adipose tissue (WAT) pads, interscapular brown adipose tissue (BAT) and liver are collected and weighed[2].

References:

[1]. Dumont Y, et al. BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y(2) receptor antagonist. Br J Pharmacol. 2000 Mar;129(6):1075-88.
[2]. Liisa Ailanen, et al. Peripherally Administered Y2-Receptor Antagonist BIIE0246 Prevents Diet-Induced Obesity in Mice With Excess Neuropeptide Y, but Enhances Obesity in Control Mice. Front Pharmacol. 2018; 9: 319.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
246146-55-4
同义词
AR-H 053591
化学名
(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
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
分子式
C49H57N11O6
分子量
896.06 g/mol
溶解性
<67.2mg/ml in DMSO; <23.55mg/ml in ethanol
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol