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Submit ReviewBIBN 4096
Description: Potent and selective CGRP antagonist
Alternative Names: Olcegepant
Chemical Name: 1-[3,5-Dibromo-N-[[4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-1-piperidinyl]carbonyl]-D-tyrosyl-L-lysyl]-4-(4-pyridinyl)-piperazine
Purity: ≥95% (HPLC)
Biological Activity for BIBN 4096
BIBN 4096 is a potent and selective CGRP receptor antagonist (IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively). Displays high affinity for human CGRP receptors (Ki = 14.4 pM); exhibits no significant affinity for 75 other receptors. BIBN 4096 improves pain symptoms in a mouse migraine model.
Technical Data for BIBN 4096
| M. Wt | 869.65 |
| Formula | C38H47Br2N9O5 |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 204697-65-4 |
| PubChem ID | 6918509 |
| InChI Key | ITIXDWVDFFXNEG-JHOUSYSJSA-N |
| Smiles | O=C(N[C@H](CC4=CC(Br)=C(O)C(Br)=C4)C(N[C@@H](CCCCN)C(N5CCN(C6=CC=NC=C6)CC5)=O)=O)N(CC3)CCC3N2CC1=CC=CC=C1NC2=O |
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 BIBN 4096
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.48 | 50 | |
| 2eq.HCl | 43.48 | 50 |
Preparing Stock Solutions for BIBN 4096
The following data is based on the product molecular weight 869.65. 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 |
|---|---|---|---|
| 0.5 mM | 2.3 mL | 11.5 mL | 23 mL |
| 2.5 mM | 0.46 mL | 2.3 mL | 4.6 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 25 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets for BIBN 4096
References for BIBN 4096
References are publications that support the biological activity of the product.
Doods et al (2000) Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br.J.Pharmacol. 129 420 PMID: 10711339
Rudolf et al (2005) Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl J.Med.Chem. 48 5921 PMID: 16161996
Prado et al (2021) TREK channel activation suppresses migraine pain phenotype. iScience 24 102961 PMID: 34458705
If you know of a relevant reference for BIBN 4096, please let us know.
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Keywords: BIBN 4096, BIBN 4096 supplier, BIBN4096, migraine, potent, selective, CGRP, receptors, antagonists, calcitonin, gene-related, peptides, Olcegepant, Calcitonin, and, Related, Receptors, 4561, Tocris Bioscience
15 Citations for BIBN 4096
Citations are publications that use Tocris products. Selected citations for BIBN 4096 include:
Prado et al (2021) TREK channel activation suppresses migraine pain phenotype. iScience 24 102961 PMID: 34458705
Stuart B et al (2018) Reflex regulation of breathing by the paratrigeminal nucleus via multiple bulbar circuits. Brain Struct Funct 223 4005-4022 PMID: 30116890
Corey R et al (2022) Nociceptor neurons affect cancer immunosurveillance. Nature 611 405-412 PMID: 36323780
Kai et al (2022) Src Family Kinases Facilitate the Crosstalk between CGRP and Cytokines in Sensitizing Trigeminal Ganglion via Transmitting CGRP Receptor/PKA Pathway. Cells 11 PMID: 36359895
Shuai et al (2022) Nociceptor Neurons are Involved in the Host Response to Escherichia coli Urinary Tract Infections. J Inflamm Res 15 3337-3353 PMID: 35702548
M et al (2016) Amylin modulates the formalin-induced tonic pain behaviours in rats. Eur J Pain 20 1741-1752 PMID: 27264026
Zhen et al (2023) Lidocaine alleviates inflammation and pruritus in atopic dermatitis by blocking different population of sensory neurons. Br J Pharmacol 180 1339-1361 PMID: 36521846
Ian M et al (2023) Inhibition of CGRP signaling impairs fracture healing in mice. J Orthop Res 41 1228-1239 PMID: 36281531
Aubdool et al (2014) TRPA1 is essential for the vascular response to environmental cold exposure. Nat Commun 5 5732 PMID: 25501034
Keith M et al (2020) Paracrine signalling by cardiac calcitonin controls atrial fibrogenesis and arrhythmia. Nature 587 460-465 PMID: 33149301
Qini et al (2020) Characterization of the effects of calcitonin gene-related peptide receptor antagonist for Alzheimer's disease. Neuropharmacology 168 108017 PMID: 32113968
Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376 PMID: 24327954
Pinho-Ribeiro et al (2018) Blocking Neuronal Signaling to Immune Cells Treats Streptococcal Invasive Infection. Cell 173 1083 PMID: 29754819
Craig L et al (2021) Role of perivascular nerve and sensory neurotransmitter dysfunction in inflammatory bowel disease. Am J Physiol Heart Circ Physiol 320 H1887-H1902 PMID: 33710922
Zhao and Levy (2018) The CGRP receptor antagonist BIBN4096 inhibits prolonged meningeal afferent activation evoked by brief local K+ stimulation but not cortical spreading depression-induced afferent sensitization. Pain Rep 3 e632 PMID: 29430561
Do you know of a great paper that uses BIBN 4096 from Tocris? Please let us know.
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