For research use only. Not for therapeutic Use.
BIBP3226（Cat No.:I004235）is a selective, non-peptide antagonist of the bradykinin B2 receptor, a G-protein-coupled receptor involved in inflammation, pain, and vascular regulation. By blocking the B2 receptor, BIBP3226 can modulate bradykinin-mediated effects, including vasodilation and the release of pro-inflammatory mediators. It has been studied for its potential therapeutic applications in conditions like pain management, cardiovascular diseases, and inflammatory disorders. BIBP3226 may help alleviate symptoms related to excessive bradykinin activity, such as in conditions like hereditary angioedema, where bradykinin levels are abnormally elevated.
| Catalog Number | I004235 |
| CAS Number | 159013-54-4 |
| Synonyms | BIBP3226; BIBP 3226; BIBP-3226.;(2R)-5-(diaminomethylideneamino)-2-[[2,2-di(phenyl)acetyl]amino]-N-[(4-hydroxyphenyl)methyl]pentanamide |
| Molecular Formula | C27H31N5O3 |
| Purity | ≥95% |
| Target | Neuronal Signaling |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term or -20 °C for long term |
| IUPAC Name | (2R)-5-(diaminomethylideneamino)-2-[(2,2-diphenylacetyl)amino]-N-[(4-hydroxyphenyl)methyl]pentanamide |
| InChI | InChI=1S/C27H31N5O3/c28-27(29)30-17-7-12-23(25(34)31-18-19-13-15-22(33)16-14-19)32-26(35)24(20-8-3-1-4-9-20)21-10-5-2-6-11-21/h1-6,8-11,13-16,23-24,33H,7,12,17-18H2,(H,31,34)(H,32,35)(H4,28,29,30)/t23-/m1/s1 |
| InChIKey | KUWBXRGRMQZCSS-HSZRJFAPSA-N |
| SMILES | C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC3=CC=C(C=C3)O |
| Reference | </br>1:In vivo inhibition of neuropeptide FF agonism by BIBP3226, an NPY Y1 receptor antagonist. Fang Q, Guo J, He F, Peng YL, Chang M, Wang R.Peptides. 2006 Sep;27(9):2207-13. Epub 2006 Jun 9. PMID: 16762456 </br>2:Functional properties of Pfr(Tic)amide and BIBP3226 at human neuropeptide FF2 receptors. Engström M, Wurster S, Savola JM, Panula P.Peptides. 2003 Dec;24(12):1947-54. PMID: 15127947 </br>3:Intracerebroventricular injection of a neuropeptide Y-Y1 receptor agonist increases while BIBP3226, a Y1 antagonist, reduces the infarct volume following transient middle cerebral artery occlusion in rats. Chen SH, Cheung RT.Neuroscience. 2003;116(1):119-26. PMID: 12535945 </br>4:Effects of BIBP3226 and BIBP3435 on cytosolic calcium in neuropeptide Y Y1 receptor-transfected Chinese hamster ovary cells and wild type CHO-K1 cells. Van Liefde, Vanderheyden PM, De Backer JP, Ebinger G, Vauquelin G.J Recept Signal Transduct Res. 2001 Feb;21(1):11-23. PMID: 11693170 </br>5:Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226. Mollereau C, Gouardères C, Dumont Y, Kotani M, Detheux M, Doods H, Parmentier M, Quirion R, Zajac JM.Br J Pharmacol. 2001 May;133(1):1-4. PMID: 11325787 Free PMC Article</br>6:Neuropeptide Y Y1 receptor antagonist BIBP3226 produces conditioned place aversion in rats. Kask A, Kivastik T, Rägo L, Harro J.Prog Neuropsychopharmacol Biol Psychiatry. 1999 May;23(4):705-11. PMID: 10390728 </br>7:[3H]-BIBP3226 and [3H]-NPY binding to intact SK-N-MC cells and CHO cells expressing the human Y1 receptor. Vanderheyden PM, Van Liefde I, de Backer JP, Vauquelin G.J Recept Signal Transduct Res. 1998 Jul-Nov;18(4-6):363-85. PMID: 9879066 </br>8:Anxiogenic-like effect of the NPY Y1 receptor antagonist BIBP3226 administered into the dorsal periaqueductal gray matter in rats. Kask A, Rägo L, Harro J.Regul Pept. 1998 Sep 25;75-76:255-62. PMID: 9802417 </br>9:Effect of BIBP3226 on inositol phosphate accumulation and cytosolic calcium level in control and NPY Y1 receptor expressing CHO-K1 cells. Vanderheyden PM, Van Liefde I, DeBacker JP, Ebinger G, Vauquelin G.Regul Pept. 1998 Sep 25;75-76:191-9. PMID: 9802409 </br>10:Anticonvulsant properties of BIBP3226, a non-peptide selective antagonist at neuropeptide Y Y1 receptors. Gariboldi M, Conti M, Cavaleri D, Samanin R, Vezzani A.Eur J Neurosci. 1998 Feb;10(2):757-9. PMID: 9749738 |
