BIBO 3304 trifluoroacetate
目录号 : GC14089
An antagonist of NPY receptor Y1
Cas No.:191868-14-1,2310085-85-7
Sample solution is provided at 25 µL, 10mM.
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BIBO 3304 is a high affinity NPY Y1 receptor antagonist with IC50 values of 0.72 and 0.38 nM at rat and human receptors respectively [1].
Neuropeptide Y is a 36 amino acid polypeptide that is expressed in the hypothalamus. It is an endocrine and neuronal messenger involved in many physiological processes such as elevates blood pressure and stimulates food intake [1].
BIBO 3304 displayed high affinity (IC50=0.69+0.16 nM) for the human Y1 receptor stably expressed in BHK cells and a higher affinity(IC50=0.38+0.06 nM) for SK-N-MC cells, a human neuroblastoma cell line endogenously expressing the Y1 receptor. BIBO 3304 exhibited selective binding to the Y1 receptor subtype and more than 1000 ± 10,000-fold lower affinity for the human Y2 receptor, the human and rat Y4 receptor as well as the human and rat Y5 receptor. In SK-N-MC cells, the NPY induced inhibition of cAMP synthesis was antagonized by 100 nM BIBO 3304 with a pKb of 9.1+0.4 [1].
In a rat model, BIBO 3304 inhibited feeding response mediated by 1mg NPY in a dose-dependent way. A dose of 30mg caused an approximately 50% inhibition (1.87+0.3 g, n=18). BIBO 3304 (30mg) had no effect on noradrenaline or galanin induced feeding. However, it can block the feeding response mediated by NPY (2 ± 36) (1mg), NPY (3 ± 36) (1mg) and [Leu31, Pro34]NPY (2mg) [1]. BIBO 3304 also antagonizes anxiolytic-like effects of NPY in the basolateral nucleus of the amygdala in rats [2].
References:
[1]. Wieland HA, Engel W, Eberlein W, et al. Subtype selectivity of the novel nonpeptide neuropeptide Y Y1 receptor antagonist BIBO 3304 and its effect on feeding in rodents. Br J Pharmacol, 1998, 125(3): 549-55.
[2]. Sajdyk TJ, Vandergriff MG, Gehlert DR. Amygdalar neuropeptide Y Y1 receptors mediate the anxiolytic-like actions of neuropeptide Y in the social interaction test. Eur J Pharmacol, 1999, 5;368(2-3): 143-147.
| Cas No. | 191868-14-1,2310085-85-7 | SDF | |
| 化学名 | 2,2,2-trifluoroacetic acid compound with (R,Z)-5-guanidino-N-(4-(((hydroxy(imino)methyl)amino)methyl)benzyl)-2-((Z)-(1-hydroxy-2,2-diphenylethylidene)amino)pentanimidic acid (2:1) | ||
| Canonical SMILES | N=C(NCCC[C@](/N=C(O)/C(C1=CC=CC=C1)C2=CC=CC=C2)([H])/C(O)=N/CC3=CC=C(CNC(O)=N)C=C3)N.FC(F)(F)C(O)=O.FC(F)(F)C(O)=O | ||
| 分子式 | C29H35N7O3.2CF3CO2H | 分子量 | 757.69 |
| 溶解度 | <75.77mg/ml in DMSO; <75.77mg/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 | 1.3198 mL | 6.599 mL | 13.198 mL |
| 5 mM | 0.264 mL | 1.3198 mL | 2.6396 mL |
| 10 mM | 0.132 mL | 0.6599 mL | 1.3198 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 | ||||||||||
| 计算重置 | ||||||||||
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.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet