BIBO 3304 trifluoroacetate
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.
BIBO 3304是一种高亲和性的NPY Y1受体拮抗剂,作用于大鼠和人的受体,IC50值分别为0.72和0.38 nM[1]。
神经肽Y是36个氨基酸的多肽,在下丘脑中表达,是一种内分泌和神经元信使,参与许多生理过程,如升高血压和刺激食物摄取[1]。
BIBO 3304对在BHK细胞中稳定表达的人Y1受体具有高亲和性,IC50值为0.69+0.16 nM,而对SK-N-MC细胞(内源性表达Y1受体的人神经母细胞瘤细胞系)具有更高的亲和性,IC50值为0.38+0.06 nM。BIBO 3304与Y1受体亚型的结合具有选择性,而对人Y2受体、人和大鼠的Y4受体,以及人和大鼠的Y5受体具有超过1000 ± 10,000倍更低的亲和力。在SK-N-MC细胞中,100 nM的BIBO 3304可拮抗NPY对cAMP合成的抑制,pKb值为9.1+0.4[1]。
在大鼠模型中,BIBO 3304以剂量依赖的方式抑制1 mg NPY介导的喂养响应,30 mg的剂量可引起将近50%的抑制(1.87+0.3 g, n=18)。BIBO 3304可以阻断NPY(2 ± 36)(1 mg)、NPY(3 ± 36)(1 mg)和[Leu31, Pro34]NPY(2mg)介导的喂养响应。然而,BIBO 3304(30mg)对去甲肾上腺素或甘丙肽诱导的喂养没有影响[1]。在大鼠中,BIBO 3304也拮抗NPY在杏仁核的基底外侧核中的抗焦虑样作用[2]。
参考文献:
[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.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 757.69 |
Cas No. | 191868-14-1 |
Formula | C29H35N7O3·2CF3CO2H |
Solubility | <75.77mg/ml in DMSO; <75.77mg/ml in ethanol |
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) |
SDF | Download SDF |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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