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Submit ReviewBIBO 3304 trifluoroacetate
Description: Highly selective NPY Y1 receptor antagonist
Chemical Name: N-[(1R)-1-[[[[4-[[(Aminocarbonyl)amino]methyl]phenyl]methyl]amino]carbonyl]-4-[(aminoiminomethyl)amino]butyl]-α-phenyl-benzeneacetamide ditrifluoroacetate
Purity: ≥98% (HPLC)
Biological Activity for BIBO 3304 trifluoroacetate
BIBO 3304 trifluoroacetate is a high affinity NPY Y1 receptor antagonist (IC50 values are 0.38 and 0.72 nM at human and rat receptors respectively) that displays > 2600-fold selectivity over Y2, Y4 and Y5 receptors. Inhibits NPY- and fasting-induced feeding in vivo following central administration. Also antagonizes anxiolytic-like effects of NPY.
Compound Libraries for BIBO 3304 trifluoroacetate
BIBO 3304 trifluoroacetate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for BIBO 3304 trifluoroacetate
| M. Wt | 757.69 |
| Formula | C29H35N7O3.2CF3CO2H |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2310085-85-7 |
| PubChem ID | 5311022 |
| InChI Key | TVMJSGGZULFVCZ-XMMPIXPASA-N |
| Smiles | OC(=O)C(F)(F)F.OC(=O)C(F)(F)F.NC(=N)NCCC[C@@H](NC(=O)C(C1=CC=CC=C1)C1=CC=CC=C1)C(=O)NCC1=CC=C(CNC(N)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for BIBO 3304 trifluoroacetate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 75.77 | 100 | |
| ethanol | 15.15 | 20 |
Preparing Stock Solutions for BIBO 3304 trifluoroacetate
The following data is based on the product molecular weight 757.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.32 mL | 6.6 mL | 13.2 mL |
| 5 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 10 mM | 0.13 mL | 0.66 mL | 1.32 mL |
| 50 mM | 0.03 mL | 0.13 mL | 0.26 mL |
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Product Datasheets for BIBO 3304 trifluoroacetate
References for BIBO 3304 trifluoroacetate
References are publications that support the biological activity of the product.
Wieland et al (1998) Subtype selectivity of the novel nonpeptide neuropeptide Y Y1 receptor antagonist BIBO 3304 and its effect on feeding in rodents. Br.J.Pharmacol. 125 549 PMID: 9806339
Sajdyk et al (1999) Amygdalar neuropeptide Y Y1 receptors mediate the anxiolytic-like actions of neuropeptide Y in the social interaction test. Eur.J.Pharmacol. 368 143 PMID: 10193650
Lecklin et al (2002) Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br.J.Pharmacol. 135 2029 PMID: 11959807
If you know of a relevant reference for BIBO 3304 trifluoroacetate, please let us know.
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Keywords: BIBO 3304 trifluoroacetate, BIBO 3304 trifluoroacetate supplier, selective, NPY, Y1, receptor, antagonists, Neuropeptide, Y, Receptors, BIBO3304, trifluoroacetate, neuropeptides, 2412, Tocris Bioscience
11 Citations for BIBO 3304 trifluoroacetate
Citations are publications that use Tocris products. Selected citations for BIBO 3304 trifluoroacetate include:
Panaro et al (2014) The melanocortin-4 receptor is expressed in enteroendocrine L cells and regulates the release of peptide YY and glucagon-like peptide 1 in vivo. Neuropsychopharmacology 20 1018 PMID: 25453189
Pickens et al (2009) Effect of pharmacological manipulations of neuropeptide Y and corticotropin-releasing factor neurotransmission on incubation of conditioned fear. Neuroscience 164 1398 PMID: 19800945
Sanchez et al (2021) Photo-induced receptor confinement drives ligand-independent GPCR signaling. Science 371 PMID: 33632896
Chen et al (2012) Activation of NPY receptors suppresses excitatory synaptic transmission in a taste-feeding network in the lower brain stem. Am J Physiol Regul Integr Comp Physiol 302 R1401 PMID: 22513746
Kojima et al (2012) A role for endogenous peptide YY in tachykinin NK(2) receptor-triggered 5-HT release from guinea pig isolated colonic mucosa. Br J Pharmacol 167 1362 PMID: 22758653
Choi et al (2019) Elevated Neuropeptide Y in Endothelial Dysfunction Promotes Macrophage Infiltration and Smooth Muscle Foam Cell Formation. Front Immunol 10 1701 PMID: 31379881
Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Cell Metab 488 172 PMID: 22801496
Maymon et al (2019) Neuropeptide Y and cannabinoids interaction in the amygdala after exposure to shock and reminders model of PTSD Neuropharmacology 162 PMID: 31622603
Alhadeff et al (2018) A Neural Circuit for the Suppression of Pain by a Competing Need State. Cell 173 140 PMID: 29570993
Cohen et al (2015) Diurnal fluctuations in HPA and neuropeptide Y-ergic systems underlie differences in vulnerability to traumatic stress responses at different zeitgeber times. J Neurosci 40 774 PMID: 25241802
Martins et al (2015) Activation of Neuropeptide Y Receptors Modulates Retinal Ganglion Cell Physiology and Exerts Neuroprotective Actions In Vitro. ASN Neuro 7 PMID: 26311075
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.