Olcegepant

• UNSPSC 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].

• Target Antigen:

  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 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.Adv Sci (Weinh). 2024 Jun 14:e2400242.|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. 2023 Oct 24.|Int Immunopharmacol. 2024 Mar 6:130:111766.|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. July 13, 2021.|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.|Vascul Pharmacol. 2017 Mar;90:36-43.|Adv Sci (Weinh). 2021 Oct 28;e2103005.|Cephalalgia. 2020 Aug;40(9):924-934.|Cephalalgia. 2021 Mar;41(3):329-339.|Cephalalgia. 2019 Dec;39(14):1827-1837. |J Headache Pain. 2022 Mar 8;23(1):35.|Journal of Traditional Chinese Medical Sciences. 21 June 2022.|Sci Rep. 2018 Jan 30;8(1):1836.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 2

• CAS Number:

  204697-65-4