BIBN 4096

Cat. No. 4561

BIBN 4096 C38H47Br2N9O5 [204697-65-4]

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Alternative Name: 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

Biological Activity

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.

Technical Data

M.Wt:
869.65
Formula:
C38H47Br2N9O5
Solubility:
Soluble to 50 mM in DMSO and to 50 mM in 2eq.HCl
Purity:
>96 %
Storage:
Store at -20°C
CAS No:
204697-65-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J.Med.Chem. 48 5921. PMID: 16161996.

Doods et al (2000) Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br.J.Pharmacol. 129 420. PMID: 10711339.

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Citations are publications that use Tocris products. Selected citations for BIBN 4096 include:

Aubdool et al (2014) TRPA1 is essential for the vascular response to environmental cold exposure. Nat Commun 5 5732. PMID: 25501034.

Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376. PMID: 24327954.

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Keywords: BIBN 4096, supplier, BIBN4096, migraine, potent, selective, CGRP, receptors, antagonists, calcitonin, gene-related, peptides, Olcegepant, Tocris Bioscience, Calcitonin and Related Receptor Antagonist products

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