| Name | Olcegepant |
| Description | Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP). |
| In vitro | Olcegepant exhibits exceptional efficacy at primate CGRP receptors, demonstrating a high affinity (Ki) of 14.4±6.3 (n=4) pM for human CGRP receptors, surpassing that of the endogenous ligand CGRP and demonstrating a 150-fold greater affinity than the peptidic antagonist CGRP8-37. It competitively antagonizes CGRP-induced concentration-dependent relaxation, effectively reversing CGRP-mediated vasodilation in human cerebral vessels and inhibiting neurogenic vasodilation in a surrogate animal model for migraine pathophysiology. This suggests that Olcegepant, acting as a CGRP receptor antagonist, may be a potential novel abortive treatment for migraines. Its competitive antagonism has also been confirmed in SK-N-MC cells, with its effects observed in isolated human cerebral, coronary, and omental arteries using sensitive myograph techniques[1][2][3]. |
| In vivo | Pre-treatment with Olcegepant (900 μg/kg) inhibits capsaicin-induced Fos expression in the spinal trigeminal nucleus by 57%, without altering phosphorylated extracellular signal-regulated kinase expression in the trigeminal ganglion. Olcegepant (1-30 μg/kg, i.v.) suppresses CGRP effects on facial blood flow in marmosets and significantly reduces mechanical allodynia in CCI-ION rats (0.3-0.9 mg/kg, i.v.). Additionally, Olcegepant (0.6 mg/kg, i.v.) decreases c-Fos immunolabeled cells and ATF3 transcript upregulation, but not interleukin-6, in the trigeminal ganglion of CCI-ION rats [2][4][5]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 23.81 mg/mL (27.38 mM), Sonication is recommended.
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| Keywords | inhibit | BIBN 4096 | Olcegepant | BIBN4096 | CGRP Receptor | Calcitonin gene-related peptide receptor | Inhibitor |
| Inhibitors Related | HCGRP-(8-37) acetate | Ubrogepant | Rimegepant | Vazegepant hydrochloride | Vazegepant | CGRP 8-37 (rat) | β-CGRP, human acetate | Calcitonin（salmon） Acetate(47931-85-1(free base)) | Galcanezumab | Calcitonin (salmon) | Erenumab | CGRP antagonist 1 |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Ion Channel Targeted Library | Anti-Cancer Drug Library |
United States
