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Olcegepant

CAT: 0804-HY-10095-01Size: 2 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-10095-01Size:2 mg
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Description
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP[1][2].
CAS Number
204697-65-4
Product Name Alternative
BIBN-4096; BIBN 4096BS
UNSPSC
12352005
Target
CGRP Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/Olcegepant.html
Purity
99.83
Solubility
DMSO : ≥ 50 mg/mL
Smiles
O=C1N(CC2=C(N1)C=CC=C2)C3CCN(C(N[C@@H](C(N[C@H](C(N4CCN(C5=CC=NC=C5)CC4)=O)CCCCN)=O)CC6=CC(Br)=C(C(Br)=C6)O)=O)CC3
Molecular Formula
C38H47Br2N9O5
Molecular Weight
869.65
References & Citations
[1]Rudolf K, et al. 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. 2005 Sep 22;48 (19) :5921-31.|[2]Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129 (3) :420-3.|[3]Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434 (1-2) :49-53.|[4]Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132 (Pt 11) :3134-41.|[5]Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153 (9) :1939-48.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Citation 01
Adv Sci (Weinh) . 2024 Jun 14:e2400242.|Adv Sci (Weinh) . 2025 Apr;12 (14) :e2409251.|Biomed Pharmacother. 2025 Aug:189:118344.|Biomed Res Int. 2022 Jun 16;2022:1585840.|Br J Pharmacol. 2024 May 7.|Cell Mol Life Sci. 2024 Aug 28;81 (1) :373.|Cell Physiol Biochem. 2017;41 (4) :1457-1467. |Cell Rep. 2024 Oct 15;43 (10) :114859.|Cell. 2024 Jun 6;187 (12) :2935-2951.e19.|Cephalalgia. 2024 Jul;44 (7) :3331024241254088.|Department of Biology, Chemistry, Pharmacy. 2020 Oct.|Freie Universitt Berlin. 2021 Feb.|Front Cell Neurosci. 2018 Sep 11:12:304.|Int Endod J. 2024 Jan;57 (1) :37-49.|Int Immunopharmacol. 2024 Mar 30:130:111766.|Int J Mol Sci. 2019 Nov 20;20 (23) :5826.|J Headache Pain. 2022 Sep 30;23 (1) :128.|J Headache Pain. 2024 Aug 21;25 (1) :136.|J Headache Pain. 2024 Oct 10;25 (1) :176.|J Invest Dermatol. 2019 Mar;139 (3) :656-664.|Korean J Pain. 2022 Apr 1;35 (2) :173-182.|Nat Med. 2016 Oct;22 (10) :1160-1169. |Neuropeptides. 2015 Aug;52:31-7. |Orthop J Sports Med. 2021 Jul 13;9 (7) :23259671211003982.|Peptides. 2021 Jan;135:170423.|Research Square Print. August 19th, 2022.|Sci Rep. 2020 Jul 10;10 (1) :11408.|Sci Rep. 2022 Aug 16;12 (1) :13894.|Small Methods. 2024 Aug 1:e2400216.|Tissue Cell. 2025 Nov 21:99:103243.|Vascul Pharmacol. 2017 Mar:90:36-43.|Adv Sci (Weinh) . 2021 Oct 28; e2103005.|Cephalalgia. 2019 Dec;39 (14) :1827-1837.|Cephalalgia. 2020 Aug;40 (9) :924-934.|Cephalalgia. 2021 Mar;41 (3) :329-339.|J Headache Pain. 2022 Mar 8;23 (1) :35.|J Tradit Chinese Medical Sci. 21 June 2022.|Sci Rep. 2018 Jan 30;8 (1) :1836.

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