BIBN 4096

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BIBN 4096 | CAS No. 204697-65-4 | Calcitonin and Related Receptor Antagonists
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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%

Product Details
Citations (15)
Supplemental Products

Biological Activity

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

Soluble to 50 mM in DMSO and to 50 mM in 2eq.HCl
Store at -20°C

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.

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Citations for BIBN 4096

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

15 Citations: Showing 1 - 10

  1. Inhibition of CGRP signaling impairs fracture healing in mice.
    Authors: Ian M Et al.
    J Orthop Res  2023;41:1228-1239
  2. Lidocaine alleviates inflammation and pruritus in atopic dermatitis by blocking different population of sensory neurons.
    Authors: Zhen Et al.
    Br J Pharmacol  2023;180:1339-1361
  3. Nociceptor neurons affect cancer immunosurveillance.
    Authors: Corey R Et al.
    Nature  2022;611:405-412
  4. Nociceptor Neurons are Involved in the Host Response to Escherichia coli Urinary Tract Infections.
    Authors: Shuai Et al.
    J Inflamm Res  2022;15:3337-3353
  5. Src Family Kinases Facilitate the Crosstalk between CGRP and Cytokines in Sensitizing Trigeminal Ganglion via Transmitting CGRP Receptor/PKA Pathway.
    Authors: Kai Et al.
    Cells  2022;11
  6. Role of perivascular nerve and sensory neurotransmitter dysfunction in inflammatory bowel disease.
    Authors: Craig L Et al.
    Am J Physiol Heart Circ Physiol  2021;320:H1887-H1902
  7. TREK channel activation suppresses migraine pain phenotype.
    Authors: Prado Et al.
    iScience  2021;24:102961
  8. Paracrine signalling by cardiac calcitonin controls atrial fibrogenesis and arrhythmia.
    Authors: Keith M Et al.
    Nature  2020;587:460-465
  9. Characterization of the effects of calcitonin gene-related peptide receptor antagonist for Alzheimer's disease.
    Authors: Qini Et al.
    Neuropharmacology  2020;168:108017
  10. The CGRP receptor antagonist BIBN4096 inhibits prolonged meningeal afferent activation evoked by brief local K+ stimulation but not cortical spreading depression-induced afferent sensitization.
    Authors: Zhao and Levy
    Pain Rep  2018;3:e632


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