Molecular Formula | C31H36F3N7O5 |
Molar Mass | 643.67 |
Solubility | Soluble in DMSO |
Storage Condition | Store at +4°C |
Use | BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively) |
Reference Show more | 1: Shi Z, Li B, Brooks VL. Role of the Paraventricular Nucleus of the Hypothalamus in the Sympathoexcitatory Effects of Leptin. Hypertension. 2015 Nov;66(5):1034-41. doi: 10.1161/HYPERTENSIONAHA.115.06017. Epub 2015 Sep 14. PubMed PMID: 26370892; PubMed Central PMCID: PMC4798233. 2: Wierońska JM, Smiałowska M, Brański P, Gasparini F, Kłodzińska A, Szewczyk B, Pałucha A, Chojnacka-Wójcik E, Pilc A. In the amygdala anxiolytic action of mGlu5 receptors antagonist MPEP involves neuropeptide Y but not GABAA signaling. Neuropsychopharmacology. 2004 Mar;29(3):514-21. PubMed PMID: 14666119. 3: Crnkovic S, Egemnazarov B, Jain P, Seay U, Gattinger N, Marsh LM, Bálint Z, Kovacs G, Ghanim B, Klepetko W, Schermuly RT, Weissmann N, Olschewski A, Kwapiszewska G. NPY/Y₁ receptor-mediated vasoconstrictory and proliferative effects in pulmonary hypertension. Br J Pharmacol. 2014 Aug;171(16):3895-907. doi: 10.1111/bph.12751. PubMed PMID: 24779394; PubMed Central PMCID: PMC4128051. 4: Wierońska JM, Stachowicz K, Kłodzińska A, Smiałowska M, Pilc A. Intraamygdaloid administration of BIBO 3304 increases water intake and extends anxiolytic effects. Pol J Pharmacol. 2004 Nov-Dec;56(6):867-70. PubMed PMID: 15662103. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.888 ml | 9.441 ml | 18.881 ml |
5 mM | 0.378 ml | 1.888 ml | 3.776 ml |
10 mM | 0.189 ml | 0.944 ml | 1.888 ml |
5 mM | 0.038 ml | 0.189 ml | 0.378 ml |
biological activity | BIBO3304 TFA is a potent, orally active, selective neuropeptide Y (NPY) y1 receptor antagonist with high affinity for both human and rat Y1 receptors (IC50 0.38 and 0.72 nM, respectively). |
Animal Model: | Adult male Chbb:Thom rats weighing between 300 and 340 g 7-week-old C57BL/6JAusb mice |
Dosage: | 30 μg 0.5 μM |
Administration: | bilateral paraventricular nucleus injection p.o. |
Result: | Attenuated the hyperphagia following fasting, especially during the first 2 h of refeeding. Significantly increased serum insulin levels. |