Catalog Number: 4561
Alternate 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
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:
    >95%
  • 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.
Background References
  1. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist.
    Doods et al.
    Br.J.Pharmacol., 2000;129:420
  2. 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
    Rudolf et al.
    J.Med.Chem., 2005;48:5921
Citations:

The citations listed below are publications that use Tocris products. Selected citations for BIBN 4096 include:

2 Citations: Showing 1 - 2
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  1. TRPA1 is essential for the vascular response to environmental cold exposure.
    Authors: Aubdool Et al.
    Nat Commun 2014;5:5732
  2. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
    Authors: Engelstoft Et al.
    Mol Metab 2013;2:376

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