Olcegepant

59,00 €

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ArtNr	HY-10095-2mg
Hersteller	MedChem Express
CAS-Nr.	204697-65-4
Menge	2 mg
Kategorie	Oncology Neuroscience Neural Lineage Markers Targets for Rodent Neurosciences Aging & Neurological Disorders Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Thyroid Cancer Neuronal Cell Markers
Typ	Inhibitors
Specific against	other
Purity	99.50
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. [1]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. [2]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. [3]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. [4]Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. [5]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.
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	BIBN-4096; BIBN 4096BS
Lieferbar
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].
StorageTemperature	-20°C, 3 years; 4°C, 2 years (Powder)
Shipping	Room Temperature
Manufacturers Applications	Neuroscience-Neuromodulation
Molecular Weight	869.65
Clinical Information	Phase 2
Solubility	1M HCl : 50 mg/mL (ultrasonic; adjust pH to 1 with HCl)\|DMSO : ≥ 50 mg/mL
Pathway	GPCR/G Protein; Neuronal Signaling
Manufacturers Product type	Reference compound

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