BIBO 3304 trifluoroacetate |
| رقم الكتالوجGC14089 |
NPY Y1 receptor antagonist,highly selective
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C29H35N7O3.2CF3CO2H | M.Wt | 757.69 |
| الذوبان | <75.77mg/ml in DMSO; <75.77mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3198 mL | 6.599 mL | 13.198 mL |
| 5 mM | 264 μL | 1.3198 mL | 2.6396 mL |
| 10 mM | 132 μL | 659.9 μL | 1.3198 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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