BIIE 0246
(Synonyms: AR-H 053591) 目录号 : GC17424
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。
Cas No.:246146-55-4
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 246146-55-4 | SDF | |
| 别名 | 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 | ||
| 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 | ||
| 分子式 | C49H57N11O6 | 分子量 | 896.06 |
| 溶解度 | <67.2mg/ml in DMSO; <23.55mg/ml in ethanol | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.116 mL | 5.58 mL | 11.16 mL |
| 5 mM | 0.2232 mL | 1.116 mL | 2.232 mL |
| 10 mM | 0.1116 mL | 0.558 mL | 1.116 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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