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Olcegepant
$60 – $610
Products Details
Product 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].
Web ID
– HY-10095
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C38H47Br2N9O5
Citations
– Biomed Res Int. 2022 Jun 16;2022:1585840.|Cell Physiol Biochem. 2017;41(4):1457-1467. |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 J Mol Sci. 2019 Nov 20;20(23):5826.|J Headache Pain. 2022 Sep 30;23(1):128.|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.|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.
References
– [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.
CAS Number
– 204697-65-4
Molecular Weight
– 869.65
Compound Purity
– 99.50
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
Clinical Information
– Phase 2
Research Area
– Neurological Disease
Solubility
– 1M HCl : 50 mg/mL (ultrasonic;adjust pH to 1 with HCl)|DMSO : ≥ 50 mg/mL
Target
– CGRP Receptor
Pathway
– GPCR/G Protein;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
